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Volume 26, Issue 10
Displaying 1-50 of 58 articles from this issue
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AKIRA MIZUTANI, IKUKATSU SUZUKI, YASUYO OHBA, TATSUKO NAKAMURA, SHIGER ...1978 Volume 26 Issue 10 Pages 2927-2932
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe hypocalcemic substance P-MSY (M.W.66000) and a few partial purified products obtained through the glacial acetic acid extraction of bovine parotid extract were examined for immune competence. Lymphocytes/polymorphs ratio increasing action was examined using the littermates of Swiss-Webster strain mice, and plaque-forming cells increasing action and rosette-forming cells increasing action were done using those of ICR strain mice. By the dosage of 0.1 μg/mouse, the sample P-MSY produced L/P ratio of 2.72±0.12, and the effect was significant at 1% level of significance against the control group. PFC and RFC activities were significant at below 5% level of significance against the respective control group in a dose of 2.5 μg/mouse (PFC/106 cells : 53.57±14.57, RFC/106 cells : 13854±2156). From these results, L/P activity of P-MSY was increased by about 2000 times that of acetone-dried powder PAI, starting materials, and the increases in PFC and RFC activities were both about 80 times. Through the assay of P-MSY and partial purified products, a tendency to increase in L/P, PFC, and RFC activities was found in proportion of hypocalcemic activity. The regression of L/P and PFC activities against log doses were examined, and it was concluded that each response revolved to a line over a moderate range of doses. Meanwhile, P-MSY was compared with the series of other products from thymus.View full abstractDownload PDF (809K) -
TADASHI SATO, HIROSHI YAMAUCHI, YOSHITAKE OGATA, MASAHIKO TSUJII, TOSH ...1978 Volume 26 Issue 10 Pages 2933-2940
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS1α-Hydroxyvitamin D3 (XIVa) was synthesized from cholesterol (Ia) in ca. 1.5% overall yield. 1α, 2α-Epoxycholest-4-en-3-one (IVa) readily obtained from Ia was converted to 1α, 2α-epoxycholest-5-en-3-one (Va) by the modified deconjugation reaction with t-BuOK in DMSO. Reduction of Va with Ca (BH4)2 and then with LiAlH4 gave 1α-hydroxycholesterol (VIIIa) in 15.6% yield from Ia. Allylic bromination and subsequent dehydrobromination of the diacetate of VIIIa afforded 1α, 3β-diacetoxycholesta-5, 7-diene (XIa), whose saponification gave the corresponding diol (XIIa). 1α-Hydroxyprovitamin D3 (XIIa) in ethanol was irradiated with the ultraviolet lights in the range between 275 and 310 nm through a newly found filter solution. The formed 1α-hydroxyprevitamin D3 (XIIIa) was thermally isomerized into 1α-hydroxyvitamin D3. The yield of XIVa from XIIa was ca. 25%. These procedures were applied to 25-hydroxycholesterol (Ib) and 1α, 25-dihydroxyvitamin D3 (XIVb) was obtained ca. 0.4% overall yield from Ib.View full abstractDownload PDF (1135K) -
SYOICHI SHIROTAKE, TAKEICHI SAKAGUCHI1978 Volume 26 Issue 10 Pages 2941-2951
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe new 2 : 1 guaninium-zinc chloride, 2 : 1 cytosinium-zinc chloride, 1 : 1 cytosine-zinc hydroxy chloride, or 2 : 1 cytosine-zinc chloride complex was obtained from a diluted hydrochloric acid, 70% ethanol, or ethanol solution. The infrared and proton magnetic resonance spectra of these complexes were characterized to assign the binding site of zinc to guanine or cytosine. On the basis of these data, it was suggested that the N9 site of guanine was bound to zinc in the guaninium-zinc chloride complex, and that the N3 site of cytosine was coordinated with zinc in the 2 : 1 cytosine-zinc chloride and 1 : 1 cytosine-zinc hydroxy chloride. It was indicated that the N3 site of cytosine was protonated in the 2 : 1 cytosinium-zinc chloride complex.View full abstractDownload PDF (1079K) -
NAOKI NAMBU, MICHITOSHI SHIMODA, YASUYUKI TAKAHASHI, HARUHISA UEDA, TS ...1978 Volume 26 Issue 10 Pages 2952-2956
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFreeze-dried inclusion compounds of nonsteroidal antiinflammatory drugs with β-cyclodextrin were administered orally to rabbits and beagle dogs in comparison with simply freeze-dried drugs. The antiinflammatory drugs used were flufenamic acid, ibuprofen, ketoprofen and indomethacin. Freeze-dried inclusion compounds showed higher levels of blood concentration and cumulative urinary excretion compared with simply freeze-dried drugs, except for indomethacin. In general, freeze-dried inclusion compounds of drugs with β-cyclodextrin showed a high dissolution rate and high bioavailability. As an exceptional case, no enhancement of the bioavailability was observed in rabbits for the inclusion compound of indomethacin compared with the simply freezedried drug. A double maxima phenomenon in blood concentration was observed in the cases of flufenamic acid and indomethacin.View full abstractDownload PDF (665K) -
SHIGERU AONUMA, YASUHIRO KOHAMA, KUNIHISA AKAI, YOSHIHIKO MURAMOTO, SH ...1978 Volume 26 Issue 10 Pages 2957-2964
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSHeart component influencing the maintenances of spreading and beating of rat myocardial cells in serum-free culture was investigated. Spreading and well-spreading % of single cells cultured with sample in Eagle minimum essential medium (MEM)-0.5% bovine serum albumin for 2 days at 37°, and relative beating % and rate of single well-spreading cells incubated with sample in Eagle MEM for 1 hr at 37° were used as parameters of the maintenance activities. Culture filtrates of heart ventricle fragments cultured in Eagle MEM for 4 days at 37° significantly promoted all of 4 parameters, and precipitates salted out with 30-50% saturated ammonium sulfate from aqueous alkaline extracts of rat, bovine and rabbit ventricles had the promoting effects like culture filtrate. But extracts prepared from brain, liver, spleen, pancreas, small intestine, kidney and skeletal muscle in the same manner as done in ventricles did not affect or inhibited spreading and beating. Desalted culture filtrates and extracts of ventricles did not possess trypsin inhibitory activity. Bovine ventricle extract was fractionated for an active principle using successive chromatographies on DEAE-cellulose, Sephadex G-100 and CM-cellulose column. The isolated principle, Fr. BVP (bovine ventricle protein), was a protein possessing molecular weight of 100000 and 18 kinds of amino acids. Fr. BVP significantly maintained spreading and beating of myocardial cells in serum-free culture in a concentration of 100 μg/dish. This protein differed biologically and chemically from Fr. A, inotropic protein of bovine heart, which was effective for promoting the beating behaviors of myocardial cells cultured with serum.View full abstractDownload PDF (1127K) -
KOZO TAKAYAMA, NAOKI NAMBU, TSUNEJI NAGAI1978 Volume 26 Issue 10 Pages 2965-2970
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe dissolution profiles of the complexes of sulfamethoxazole (SMO) and sulfamonomethoxine (SMM) with 18-crown-6 (1, 4, 7, 10, 13, 16-hexaoxacyclooctadecane, 18-C-6) involving simultaneous decomplexation were investigated kinetically in detail by a dispersed amount method and a stationary disk method in comparison with those of intact SMO and SMM. The dissolution rates of the complex before and after the phase change, Rc and Ro, respectively, the saturated concentrations of complex and intact drug, Csc and Cso, respectively, the rate constant of crystallization process, kr, and the dissolution rate constant, kt, were calculated by the stationary disk method. Analyzing the values of kr and kt obtained at various temperatures, the activation energies of crystallization and dissolution process were determined. The activation energy of crystallization process seemed small compared with the past data reported on organic medicinals.View full abstractDownload PDF (656K) -
YOSHIHISA IWAMOTO, ICHIJI MIFUCHI1978 Volume 26 Issue 10 Pages 2971-2976
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn the process of isolating several antimycin-resistant mutants of Candida utilis by treatment with N-methyl-N'-nitro-N-nitrosoguanidine, we found a simple method of isolating many antimycin-resistant variants without treatment with mutagen. When cells were grown in glucose medium containing 10-6 M antimycin for more than three days at 30°, we observed the existence of some antimycin-resistant variants in the culture medium. These variants can grow in glycerol medium containing 10-6 M antimycin in which the parental strain can not grow. The results of fluctuation test strongly suggested that antimycin-resistant variants arose unperiodically by spontaneous mutation. The respiration of antimycin-resistant variants was not inhibited by 10-7 M antimycin which inhibited completely that of parental strain, but was inhibited by the higher concentrations of antimycin. Therefore, these variants do not seem to become antimycin resistant by the possession of any special antimycin-resistant respiratory chain as reported on several fungi. Some other possibilities were discussed.View full abstractDownload PDF (625K) -
HIDENORI HAYASHI, FUMIE YAMASAKI1978 Volume 26 Issue 10 Pages 2977-2982
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSCyclic adenosine 3', 5'-monophosphate (cAMP) stimulated the induction of cAMP-phosphodiesterases of the slime mold, Dictyostelium discoideum. The membrane phosphodiesterase was induced by more than 10-5 M of cAMP concentration, while the extracellular enzyme was done 3.5-times higher by 10-6 M of cAMP compared with free cAMP. The induction of the extracellular phosphodiesterase by cAMP was inhibited by EDTA, p-chloromercuribenzene sulfonate (PCMB), concanavalin A (Con A) and progesterone which all are known to cease differentiation of the slime mold. The derivation of the extracellular enzyme was also stopped by dithiothreitol which reversely accelerates development of the cells. On the other hand, Con A and dithiothreitol further stimulated the induction of the membrane phosphodiesterase by cAMP more than by cyclic nucleotide alone. Cyclic guanosine 3', 5'-monophosphate and N6, O2'-dibutyryl cyclic adenosine 3', 5'-monophosphate are known to have much less chemotaxis-characteristics of the slime mold than cAMP. These cAMP-analogs occurred the synthesises of both the membrane and the extracellular phosphodiesterases to same or more extent. When the surface of the slime mold was treated with trypsin, the induction of only extracellular phosphodiesterase by cAMP was suppressed to half. From these results, it seems that the induction of synthesis of phosphodiesterases by cAMP in the slime mold is independent of the occurrence of chemotaxis.View full abstractDownload PDF (690K) -
YOSHINOBU NAKAI, EIHEI FUKUOKA, SHINICHIRO NAKAJIMA, YOSHIMITSU IIDA1978 Volume 26 Issue 10 Pages 2983-2989
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSVolatile medicinals, naphthalene, d-camphor, and p-cresol became amorphous during grinding with microcrystalline cellulose. The medicinal of interest was retained in the ground mixture even when the mixture was heated at moderately high temperature in vacuo. The close relationship was noticed between the retentivity and the state of the medicinals (amorphous or not) in the ground mixture. The amount of the medicinal remaining in the ground mixture was influenced by the medicinal content, the grinding time, and the amount of water adsorbed. The medicinals were very rapidly released from the ground mixture into water. The mechanism for these results was discussed, based on the structure of the groud mixture proposed in the previous paper as follows : the molecules of the volatile medicinals are enclosed by the cellulose molecules that were bound by hydrogen bonds between hydroxyl radicals. The system was regarded as an "entropy frozen solution" of the medicinal in cellulose molecules. By adding water to the ground mixture, the hydrogen bonds are weakened and the medicinal molecule obtains the ability of molecular movement.View full abstractDownload PDF (844K) -
MINEO SANEYOSHI, MOTOKO INOMATA, FUMIKO FUKUOKA1978 Volume 26 Issue 10 Pages 2990-2997
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSCondensation of 2, 4-bis-trimethylsilyloxy-5-fluoropyrimidine (2a) with 1-O-acetyl-2, 3, 5-tri-O-benzoyl-β-D-ribofuranose (3a) by Friedel-Crafts catalysts has been studied. When the reaction was run in acetonitrile at room temperature for 3 hr with 1 : 1 : 1 molar ratio of the base, sugar and stannic chloride, 2', 3', 5'-tri-O-benzoyl-5-fluorouridine (4a) was obtained in an excellent yield (98%). As 1-O-acetyl sugars, 1, 2, 3, 5-tetra-O-acetyl-β-D-ribofuranose (3b), 1, 2, 3, 4, 6-penta-O-acetyl-α-D-glucopyranose (3c), and 1, 2-di-O-acetyl-3-p-toluenesulfonyl-5-O-methoxycarbonyl-D-xylofuranose (3d) could also be used in place of 3a to give the corresponding 1-β-D-glycosyl nucleosides highly stereoselectively. The same method of nucleoside synthesis was extended to the 5-fluorocytosine series to afford 5-fluorocytidine (7a) and 1-β-D-arabinofuranosyl-5-fluorocytosine (7b) in good yields starting from trimethylsilylated N4-acetyl-5-fluorocytosine (6). Additionally, 2, 4-dimethoxy-5-fluoropyrimidine (2b) could be coupled with 3a in similar conditions to give 1-(2, 3, 5-tri-O-benzoyl-β-D-ribofuranosyl)-4-methoxy-5-fluoro-1, 2-dihydropyrimidin-2-one (4e) in good yield. The antitumor activities of the various products obtained against ascites Sarcoma 180 are also described.View full abstractDownload PDF (1026K) -
EIKO OHTSUKA, EIKO NAKAGAWA, TOSHIKI TANAKA, ALEXANDERF. MARKHAM, MORI ...1978 Volume 26 Issue 10 Pages 2998-3006
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA hexanucleotide GpGpGpUpGpG corresponding to bases 5-10 of the tRNAMetf from E. coli. has been synthesized by stepwise addition of mononucleotides. The segment contained five guanine bases out of six nucleotides. We have improved the protection of the 2', 3'-hydroxyl groups of guanosine and guanosine 3'-phosphate by replacing to avoid undesirable deblocking during elongation of the chain. Condensation of 5'-O-monomethoxytrityl-2'-O-benzoyl-N-isobutyrylguanosine 3'-phosphate (9) with 2', 3'-O-dibenzoyl-N-isobutyrylguansoine (5) gave protected GpG in a yield of 62%. Subsequent addition of mononucleotides to the growing chain was performed after selective removal of the 5'-monomethoxytrityl group. Dicyclohexylcarbodiimide (DCC) was used as condensing reagent throughout the synthesis. The excess of mononucleotide and the yield in each addition reaction were as follows : UpGpG (protected) 2.2 fold, 28%, GpUpGpG (protected), 5 fold, 32% ; GpGpUpGpG (protected) 10 fold, 35% ; GpGpUpGpG, 10 fold, 12%. The protected intermediate oligomers were isolated by ion-exchange chromatography on TEAE-cellulose columns and identified by enzymatic hydrolyses after deblocking. The hexanucleotide was separated by gel filtration on Sephadex LH-20 and purified on DEAE-cellulose in the presence of 7 M urea at 55°. The circular dichroism spectra of these guanine rich ribooligomers have measured and a marked difference between the pentamer GpGpUpGpG and the hexamer GpGpUpGpG has been observed.View full abstractDownload PDF (1089K) -
SHOJI KOJIMA, MITSUO NAKAGAWA, RITSUKO SUZUKI, MICHIKO HORIO, YOHKO TA ...1978 Volume 26 Issue 10 Pages 3007-3009
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSUpon a single oral administration of 2, 6-DIPN (100mg/kg) to rats, about 85% of the dose was absorbed from the gastrointestinal tract during 48 hr after the administration. Only a small amount of unchanged 2, 6-DIPN was excreted in urine. The maximum levels of 2, 6-DIPN in the liver, kidney, heart, spleen, brain and muscle were obtained within 4 hr after the administration and then the levels decreased with time. However, the time for reaching the maximum level of 2, 6-DIPN in the skin and adipose tissue was longer than that in the other tissues. In addition, the content and disappearance of 2, 6-DIPN in the adipose tissue were higher and slower than those in the other tissues.View full abstractDownload PDF (472K) -
SHOJI YAHARA, OSAMU TANAKA, ITSUO NISHIOKA1978 Volume 26 Issue 10 Pages 3010-3016
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIsolation and structure determination of leaf-saponins of P. japonicus C.A. MEYER (Araliaceae) collected in Hiroshima-ken had already been reported. The aglycones of these saponins are represented by 20 (S)-protopanaxatriol (7) and its homologue (modification of the side chain). The present study revealed that the composition of leaf-saponins of this plant significantly depend upon the localities. From the leaves collected in Tottoriken (T-type), there were isolated two dammarane type saponins, named chikusetsusaponins-LT5 (11) and-LT8 (12), the former of which was also obtained from the leaves collected in Kyoto-shi (K-type). By means of 13C nuclear magnetic resonance spectroscopy and other physical procedures, the structures of 11 and 12 were established to be dammar-24-ene-3β, 20S-diol-3-(O-β-glucopyranoside)-20-[O-β-glucopyranosyl (1→6)-β-glucopyranoside] and dammar-24-ene-3β, 20S-diol-12-one-3, 20-di (O-β-glucopyranoside), respectively. On the other hand, the leaves collected in Niigata-ken (N-type) afforded a saponin named chikusetsusaponin-LN4 (13), the structure of which was assigned as dammar-24-ene-3β, 20S-diol-12-one-3-[O-β-xylopyranosyl (1→6)-β-glucopyranoside]-20-[O-α-arabinopyranosyl (1→6)-β-glucopyranoside]. These saponins, 11, 12, and 13 are characteristic of the leaves of T-, K-, and N-types, respectively and were not detected in the leaves collected in Hiroshima-ken (H-type), while the leaf-saponins of H-type were not isolated from the leaves of T-, K-, and N-types.View full abstractDownload PDF (887K) -
KENTARO HIRAI, TERUYUKI ISHIBA1978 Volume 26 Issue 10 Pages 3017-3022
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSReactions of 2-dialkylamino-1, 3-oxathiolium (I) with amino-nucleophiles provide simple access to a variety of heterocyclic compounds. Thiadiazines and thiazoles were readily obtained from the reaction with hydrazines and ammonia, respectively. The intermediates, which were easily converted into thiazoles, were also isolated. Study of the reaction of 1 with aromatic amines revealed the formation of ring-opened ketones and 2-arylimino-1, 3-oxathioles depending upon the reaction conditions. Reactions of I with aromatic and aliphatic amines in boiling glacial acetic acid resulted in the formation of 2-iminothiazoline derivatives.View full abstractDownload PDF (782K) -
FUMIKO ABE, TATSUO YAMAUCHI1978 Volume 26 Issue 10 Pages 3023-3027
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDigitoxigenin α-L-oleandroside and 5α-adynerin were isolated from the oven-dried leaves of Nerium odorum, and the structures were elucidated with the aid of 13C nuclear magnetic resonance and finally by the conversion into the glycoside from oleandrin and by the synthesis of 5α-adynerigenin, respectively.View full abstractDownload PDF (676K) -
SUSUMU KITAGAWA, HISASHI TANAKA1978 Volume 26 Issue 10 Pages 3028-3032
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new dithio chelate, bis (N-methyl-, N-phenyl-β-mercaptothiocinnamamido) palladium-(II) was prepared by the novel simultaneous sulfurization reaction of the carbonyl-and amide-group of N-methylbenzoylacetamide with phosphorus pentasulfide. The obtained complex was studied by infrared and mass spectral procedures. The complex did not produce pyridine clathrate unlike the cases of the palladium complexes of the N-dimethylatedligands. This is likely because the N-methylated palladium complex lacks the thioamide protons with which pyridine molecules are able to interact by forming hydrogen bonds.View full abstractDownload PDF (563K) -
HITOSHI SEKIKAWA, JUNEI FUJIWARA, TSUTOMU NAGANUMA, MASAHIRO NAKANO, T ...1978 Volume 26 Issue 10 Pages 3033-3039
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPhenytoin-polyvinylpyrrolidone (PVP) coprecipitate was prepared. The X-ray diffraction spectra indicated that phenytoin in the coprecipitate did not exhibit its crystalline property. Comparative studies were made on the in vitro dissolution and the in vivo absorption of the coprecipitate and phenytoin alone. The dissolution rate of phenytoin was markedly increased in the phenytoin-PVP coprecipitate in the pharmacopoeial disintegration media at pH 1.2 and 7.5. The concentration of phenytoin released from the coprecipitate reached supersaturation within a few minutes in dissolution studies. The solution remained supersaturated for a long period. The dissolution rate of phenytoin in the coprecipitate was greater when the ratio of drug to PVP was smaller and when PVP of smaller molecular weight was used for the preparation of the coprecipitate. In vivo absorption studies of each preparation was carried out in five subjects by measuring the urinary excretion rate of free and conjugated forms of a main metabolite, 5-(p-hydroxyphenyl)-5-phenylhydantoin. Excretion rate and cumulative amount of the metabolite excreted following the oral administration of the coprecipitate were greater than those of phenytoin alone. The plasma levels of phenytoin following the administration of the coprecipitate were almost twice as high as those of the phenytoin alone, in rabbits. It was indicated that the drug was rapidly and almost completely absorbed following oral administration of the coprecipitate.View full abstractDownload PDF (853K) -
SEIICHI UESUGI, MORIO IKEHARA1978 Volume 26 Issue 10 Pages 3040-3049
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSCarbon-13 magnetic resonance spectra of 8-substituted purine nucleotides and the corresponding parent nucleotides were measured. The 8-substituted derivatives included the 2'-, 3'-, 2', 3'-cyclic, 5'-and 3', 5'-cyclic phosphates of 8-bromoadenosine and the 5'-phosphates of 8-bromoguanosine, 8-methylinosine and 2-methylthio-8-methylinosine. All the 8-substituted nucleotides showed a characteristic upfield shift (-0.9 to -3.7 ppm) of the 2'-carbon with respect to the corresponding parent nucleotides. These results show that they take a syn conformation in aqueous solution to some extent. It was concluded from consideration of the sugar puckerings in the published PMR data that the 5'-phosphate of 8-bromoadenosine takes a more rigid syn conformation than the 2'-, 3'-and 2', 3'-cyclic phosphates. It is also suggested that 8-bromoadenosine has flexible glycosidic conformation similar to those for the latter compounds in water while in DMSO it adopts a more rigid conformation. The 5'-phosphates of the other 8-substituted nucleosides were also assumed to adopt a rigid syn conformation. The influences of various types of phosphate groups on the carbon chemical shifts are also discussed. Relatively large upfield shifts were observed for the C (4') signal of the 8-substituted 5'-nucleotides which has been assumed to be a reflection of a high population of non-gg conformations about the C (4')-C (5') bond.View full abstractDownload PDF (1222K) -
KAORU NAKAJIMA, HEIHACHIRO TAGUCHI, TOHRU ENDO, ITIRO YOSIOKA1978 Volume 26 Issue 10 Pages 3050-3057
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTwo new hydroxystilbene dimers, named scirpusin A (1) and B (12), were isolated from the rhizoma of Scirpus fluviatilis (TORR.) A. GRAY (Cyperaceae) together with two known hydroxystilbenes, resveratrol and 3, 3', 4, 5'-tetrahydroxystilbene, and four known triterpens, betulin, lupeol, betulinaldehyde and betulinic acid. The structures of scirpusin A and B were elucidated to be 1 and 12, respectively, by chemical and spectral evidence.View full abstractDownload PDF (1066K) -
IKUO UEDA, YOSHINARI SATO, SHIZUO MAENO, SUMINORI UMIO1978 Volume 26 Issue 10 Pages 3058-3070
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS8-Chloro-10-(2-dimethylaminoethoxy) dibenzo [b, f] thiepin (4) and related compounds were prepared by various methods. The results from the pharmacological investigation suggest that many of these compounds will be a kind of neuroleptics and the clinical investigation of the compounds 4 as a neuroleptic is underway.View full abstractDownload PDF (1455K) -
TORU OKUYAMA, KEIKO HOSOYAMA, YUKIO HIRAGA, GOICHI KURONO, TSUNEMATSU ...1978 Volume 26 Issue 10 Pages 3071-3074
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA novel flavonol glycoside, mp 182-184°, named asiaticalin (I) was isolated from the fresh trophophyll of Osmunda asiatica OHWI (Osmundaceae). The structure of I was established as being kaempferol 3-β-alloside. This is the first found alloside of flavonoid, 13C-nuclear magnetic resonance spectrum of I was discussed in comparison with those of kaempferol (II), and astragalin (X) isolated from the same plant.View full abstractDownload PDF (607K) -
AKIRA YAGI, NOBUYUKI OKAMURA, YASUSHI HARAGUCHI, KANJI NODA, ITSUO NIS ...1978 Volume 26 Issue 10 Pages 3075-3079
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new p-coumaroylate of maslinic acid was isolated from the fruits of Zizyphus jujuba (Rhamnaceae) together with known triterpenoid acids : betulonic, oleanonic, maslinic and 3-O-trans-p-coumaroyl maslinic acid. The structure of V was characterized to be 3-O-cis-p-coumaroyl maslinic acid on the basis of chemical and spectral evidence.View full abstractDownload PDF (781K) -
TADAKAZU MURATA, TOHRU SUGAWARA, KIYOSHI UKAWA1978 Volume 26 Issue 10 Pages 3080-3100
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSeveral new β-aminopyrroles, 3-aminoindoles, pyrido [3, 4-b] indoles, and pyrrolo-[3, 2-b] pyridines have been synthesized by a sequence of reactions involving intramolecular addition of an enamine to a cyano group. Enamine (1), prepared from tert-butyl aminocyanoacetate and cyclohexane-1, 3-dione, cyclized after substitution of the methine by ethyl bromoacetate in the presence of sodium ethoxide to afford 2-tert-butoxycarbonyl-2-ethoxycarbonylmethyl-3-imino-4-oxo-4, 5, 6, 7-tetrahydroindoline (2). Reaction of 1 with methyl vinyl ketone-sodium ethoxide furnished 3-amino-2-tert-butoxycarbonyl-4-oxo-4, 5, 6, 7-tetrahydroindole (7). Similarly, certain 3-aminopyrroles (44 and 45) and pyrrolo [3, 2-b] pyridines (51 and 52) have been synthesized from the enamine (41) prepared from acetoacetate and tert-butyl aminocyanoacetate. Enamines (70-72) obtained by condensation of ethyl acetoacetate with aminocyanoacetamides underwent cyclizations to 3-amino-2-carbamoylpyrroles (73-75) upon treatment with base. Several new 3-aminopyrroles thus prepared have been derived into new pyrrolo [3, 2-d]-(78-81) and pyrrolo-[3, 4-d] pyrimidines (90 and 91). A steric effect of the neighbouring butoxycarbonyl group in 41 has also been briefly discussed.View full abstractDownload PDF (2643K) -
MAMORU SUGIURA, MASAO ISHIKAWA, MASANORI SASAKI1978 Volume 26 Issue 10 Pages 3101-3106
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSome properties of purified leucine aminopeptidase [E.C. 3.4.1.1] from Aspergillus japonica as a metalloenzyme were investigated. Leucine aminopeptidase was inhibited by various chelating agents. The addition of Zn2+ to the ethylenediaminetetraacetic acid (EDTA)-treated leucine aminopeptidase restored the activity to nearly the original level, but Co2+ was partially effective. Kinetic studies using L-leucyl-β-naphthylamide as substrate were carried out with native leucine aminopeptidase, Zn2+ or Co2+-reactivated leucine aminopeptidase after dialysis against EDTA. Michaelis constant (Km) and activation energy (Eact) of native leucine aminopeptidase were in good agreement with those of Zn2+ reactivated leucine aminopeptidase (native leucine aminopeptidase Km : 2.5×10-4 M, Eact : 9.2×103 cal/mol, Zn2+-reactivated leucine aminopeptidase Km : 2.5×10-4 M, Eact : 9.8×103 cal/mol). In the presence of L-leucyl-β-naphthylamide, the inhibition of leucine aminopeptidase by various chelating agents and a Cd2+ decreased to an extent of 23-46%. Metal analysis indicated that the purified leucine aminopeptidase containing 1 g-atom of zinc per mol of leucine aminopeptidase, and both the activity and the zinc content were lowered when native leucine aminopeptidase was treated with EDTA or o-phenanthroline.View full abstractDownload PDF (743K) -
YASUJI YAMADA, KIYOKAZU HAGIWARA, KAZUO IGUCHI, SUKEJI SUZUKI, HONGYEN ...1978 Volume 26 Issue 10 Pages 3107-3112
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFour new cucurbitacin glucosides (named arvenin I, II, III and IV) were isolated as bitter principles of Anagallis arvensis L. (Primulaceae). On the basis of the spectral studies involving carbon-13 nuclear magnetic resonance spectra and the chemical transformations, the structures of these bitter glucosides have been established as 2-O-β-D-glucopyranosyl cucurbitacin B for arvenin I, 2-O-β-D-glucopyranosyl 23, 24-dihydrocucurbitacin B for arvenin II, 2-O-β-D-glucopyranosyl cucurbitacin D for arvenin III and 2-O-β-D-glucopyranosyl cucurbitacin R for arvenin IV, respectively. This is the first isolation of cucurbitacin glucosides from the family Primulaceae.View full abstractDownload PDF (750K) -
SHIGERU KOBAYASHI, MASARU KIHARA, YOSHINOBU YAMAHARA1978 Volume 26 Issue 10 Pages 3113-3116
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe methylenedioxy ring in piperonal (1) and its 6-substituted derivatives (5, 6, 9, and 10) was opened by heating with sodium methoxide in dimethyl sulfoxide to give the phenolic products, isovanillin (4) and its 6-substituted derivatives (7, 8, 11, and 12), respectively. Similarly, the nitro compounds (16 and 19) gave phenolic products (17 and 20, respectively) by this method. However, the ring in the compounds having methyl (compound 21), carboxyl (compound 22), methoxycarbonyl (compound 23), and amide (compound 24) groups instead of the formyl group in 1 could not be opened by this method.View full abstractDownload PDF (546K) -
AKIRA OGISO, EIICHI KITAZAWA, MASAAKI KURABAYASHI, AIYA SATO, SHUJI TA ...1978 Volume 26 Issue 10 Pages 3117-3123
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA potent antipeptic ulcer substance, acyclic diterpene alcohol, was isolated from a Thai medicinal plant identified with Croton sublyratus KURZ. The structure was determined by the spectral data and stereospecific synthesis to be (E, Z, E)-7-hydroxymethyl-3, 11, 15-trimethyl-2, 6, 10, 14-hexadecatetraen-1-ol.View full abstractDownload PDF (829K) -
TOSHIHIRO HAYASHI, MAKOTO SATO, MASAHIKO OHKI, TORAHIKO KISHIKAWA1978 Volume 26 Issue 10 Pages 3124-3134
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe metabolism of 4-ethoxy-2-methyl-5-morpholino-3 (2H)-pyridazinone (M73101) in rabbits and the pharmacological activities of metabolites were investigated. Rabbits orally received the drug in a dose of 100 mg/kg excreted ten metabolites together with unchanged drug in the urine. These metabolites were characterized by their spectrometric data (infrared, mass, ultraviolet, and nuclear magnetic resonance spectra), thin-layer chromatography and gas chromatography. Some of them were unequivocally identified by comparison with synthesized authentic samples. The following compounds were found to be present in the urine : 4-ethoxy-2-methyl-5-morpholino-3 (2H)-pyridazinone (unchanged drug), 4-hydroxy-2-methyl-5-morpholino-3 (2H)-pyridazinone (M-1), 5-bis (2-hydroxyethyl) amino-4-ethoxy-2-methyl-3 (2H)-pyridazinone (M-2), 4-ethoxy-5-[2-(β-hydroxyethyloxy) ethylamino]-2-methyl-3 (2H)-pyridazinone (M-3), 4-ethoxy-5-(2-hydroxyethylamino)-2-methyl-3 (2H)-pyridazinone (M-4), 4-ethoxy-5-(2-hydroxy-tetrahydro-1, 4-oxazin-4-yl)-2-methyl-3 (2H)-pyridazinone (M-5), 4-ethoxy-5-morpholino-3 (2H)-pyridazinone (M-6), 4-ethoxy-2-methyl-5-(3-oxotetrahydro-1, 4-oxazin-4-yl)-3 (2H)-pyridazinone (M-7), 5-(N-carboxymethyl-N-2-hydroxyethylamino)-4-ethoxy-2-methyl-3 (2H)-pyridazinone (M-8), 5-[2-(carboxymethyloxy)-ethylamino]-4-ethoxy-2-methyl-3 (2H)-pyridazinone (M-9), 5-carboxymethylamino-4-ethoxy-2-methyl-3 (2H)-pyridazinone (M-10). From these results, it was concluded that the major metabolic route in rabbits was oxidative cleavage of C-N and C-O of morpholino group followed by further degradation. Deethylation and demethylation were found to be minor reaction. In the pharmacologocal studies of metabolites, no activities were observed, which indicated that the pharmacological activities of M73101 were not due to these urinary metabolites.View full abstractDownload PDF (1144K) -
TOMOO TANAKA1978 Volume 26 Issue 10 Pages 3135-3138
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA spectrophotometric method for the determination of micro-amount of osmium with thiopyrine was established, based on the formation of water-soluble bluish green complex, which shows an absorption maximum at 740 nm. The absorbance of the complex was constant over the pH range of 0.5-1.8. The addition of 2-propanol was effective to increase and maintain the absorbance. The method was satisfactorily applied to the concentration less than 20 μg/ml. The molar absorptivity was found to be 1.20×104 1·cm-1·mol-1. Various common foreign ions and other noble metal ions hardly interfered the determination. The isolated complex was confirmed to be hexakis (thiopyrine)-osmium (IV) perchlorate, by elementary analysis and the molar conductivity determined in acetonitrile.View full abstractDownload PDF (520K) -
TOMOO TANAKA1978 Volume 26 Issue 10 Pages 3139-3143
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSWhen an aqueous solution containing mercury (II), thiopyrine and eosine was shaken with 1, 2-dichloroethane at pH 10, an ion pair formed from cationic mercury (II)-thiopyrine complex and anionic eosine was extracted into the organic phase. Based on this reaction, a sensitive extraction-spectrophotometric determination method for trace of mercury was established by the absorbance measurement at 540 nm. This method is applicable to the determination of mercury less than 2.5 μg/ml. Various common cations and anions except for silver (I) and iodide did not interfere the determination practically. Molar ratio of mercury (II) to thiopyrine and eosine was found to be 1 : 2 : 1 by the continuous variation method.View full abstractDownload PDF (570K) -
HIROSHI OGAWA, TAKASHI SASAKI, HIROSHI IRIE, HARUAKI YAJIMA1978 Volume 26 Issue 10 Pages 3144-3149
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFour by-products formed during the treatment of Z (OMe)-Trp-OH with trifluoroacetic acid were isolated and their structures were assigned by nuclear magnetic resonance and mass spectra. It was found that the major by-product was H-Trp (2'-p-methoxybenzyl)-OH. Confirmatively, H-Trp (1'-tert-butyl)-OH was identified as the major by-product from Boc-Trp-OH. Such side reaction was found to be efficiently suppressed by the use of the scavenger system, such as, thioanisole containing 2% ethanedithiolskatole or dimethylsulfide containing 2% ethanedithiol-skatole, during the deprotection with trifluoroacetic acid or preferably with 4N ethanesulfonic acid.View full abstractDownload PDF (766K) -
SANGWON KIM, YUKIHIDE BANDO, NOBUKO TAKAHASHI, ZENICHI HORII1978 Volume 26 Issue 10 Pages 3150-3153
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe total synthesis of dl-anhydrolycodoline is reported. The amino-ketone (3), obtained from the amine (4) in four steps, was treated with acrylyl chloride to give the amide (1). Unfortunately, the intramolecular Michael-type cyclization of 1 to the lactam (9) for lycodoline did not take place for a stereoelectronic reason. Dehydration of 1 with conc. sulfuric acid afforded the anhydro-amide (10), which was cyclized in the presence of sodium ethoxide and dicyclohexyl-18-crown-6 to give the tetracyclic lactam (11) in a moderate yield. Reduction of 11 with lithium aluminum hydride followed by oxidation with Jones reagent afforded dl-anhydrolycodoline.View full abstractDownload PDF (650K) -
FUMIO YONEDA, MITSUKO NOGUCHI, MITSUE NODA, YOSHIHIRO NITTA1978 Volume 26 Issue 10 Pages 3154-3160
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS6-Benzylidenehydrazino-3-methyluracils were treated with sodium nitrite in acetic acid to give the corresponding 5-nitrosouracils. Dehydrative cyclization of the 5-nitrosouracils with acetic anhydride afforded 6-substituted 3-methyl-7-azalumazines, ethylation of which gave 6-substituted 1-ethyl-3-methyl-7-azalumazines. Treatment of these 7-azalumazines thus obtained and 6-substituted 1, 3-dimethyl-7-azalumazines with alcoholic sodium hydroxide caused a benzilic acid type rearrangement followed by decarboxylation and oxidation by air to give the respective 5H-imidazo [4, 5-e]-as-triazine-6 (7H)-ones (6-azapurines). Prolonged hydrolysis of 3-substituted 7-ethyl-5-methyl-5H-imidazo [4, 5-e]-as-triazine-6 (7H)-ones with alcoholic sodium hydroxide caused the ring cleavage to give 3-substituted 6-ethylamino-5-methylamino-as-triazines, which were fused with benzamidine hydrochloride to give rise to 3-substituted 7-ethyl-6-phenylimidazo [4, 5-e]-as-triazines.View full abstractDownload PDF (728K) -
TAKAO OHYASHIKI, TETSURO MOHRI1978 Volume 26 Issue 10 Pages 3161-3166
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe micelle formation of sodium dodecyl sulfate (SDS) was studied using pyrene as a fluorescence probe. The critical micelle concentration (CMC) of SDS was estimated to be 8 mM from the changes in monomer fluorescence intensity and ratio of fluorescence intensities at 392 and 375 nm, in good agreement with the reported values obtained from different methods. The results of measurements of excimer fluorescence and fluorescence polarization suggested that the small aggregates of SDS molecules are formed in their low concentrations below the CMC and that the flexibility of hydrocarbon chains in soap molecules is remarkably reduced by growing from aggregates to micelles. The difference in arrangement of hydrocarbon chains between the premicellar and micellar states were manifested also by the different responses of fluorescence parameters of pyrene to MgCl2 and temperature in low and high concentrations of SDS.View full abstractDownload PDF (688K) -
SHINZO TAMURA, MACHIKO ONO1978 Volume 26 Issue 10 Pages 3167-3177
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSHeterocyclic analogs of β-arylaminoacrolein were synthesized from corresponding heterocyclic amino compounds and malonaldehyde derivatives. The difference between the reactions of malonaldehyde with 4-aminopyridine (V) and with other aromatic primary amines was discussed.View full abstractDownload PDF (1158K) -
HIROSHI MORIYA, YOSHIHIRO FUKUOKA, YOSHIO HOJIMA, CHIAKI MORIWAKI1978 Volume 26 Issue 10 Pages 3178-3185
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSKallikreins A and B isolated from hog pancreas showed vasodilator activities of 1350 and 1450 KU/mg (weight) respectively, and same esterolytic activity of 111 units/mg toward BzArgOEt. The sugar content of kallikrein B was roughly twice as much as that of kallikrein A in neutral hexose and glucosamine. Micro-heterogeneous forms B-2 and B-3 which are comprised in kallikrein B showed a 10 times difference in sialic acid content according to their acidities observed in isoelectric focusing. From these and other results obtained by gel plate isoelectric focusing, including the treatment with neuraminidase, it is suggested that the relative acidities on the electrophoresis of various forms of hog pancreatic kallikrein are depending upon the relative amounts of sialic acid and glucosamine in their molecules.View full abstractDownload PDF (1149K) -
TAKEFUMI MOMOSE, TAKESHI NAKAMURA, KENICHI KANAI1978 Volume 26 Issue 10 Pages 3186-3188
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSβ-Apoplicatitoxin trimethyl ether (8) was synthesized by selective photocyclization of a dibenzylidenebutyrolactone (6). The photocyclization was preliminarily examined in various solvents by use of a model compound (1), and the total yield of resulting isomeric β-apolignans (2a and 2b) and the ratio of 2a/2b were shown to increase with increasing solvent polarity.View full abstractDownload PDF (504K) -
KAZUO ITO, JENGSHIOW LAI, KOJI USUDA1978 Volume 26 Issue 10 Pages 3189-3194
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFrom the methanolic extracts of Marsdenia formosana MASAMUNE (Asclepiadaceae), three new steroidal glycosides, MF-A, MF-C and MF-D, together with β-sitosterol-3β-D-glucoside (VIII) and dehydrotomentosin (I) were isolated. As the results of spectroscopic and chemical investigations, it has been demonstrated that the stereostructures of MF-A, MF-C and MF-D were represented, respectively, by the formulas II, IV and VI.View full abstractDownload PDF (817K) -
TAKEFUMI MOMOSE, KENICHI KANAI, KUMIKO HAYASHI1978 Volume 26 Issue 10 Pages 3195-3198
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe concurrent synthesis of justicidin B (3) and diphyllin (4) coexistent in Justicia procumbens var. leucantha and of taiwanin C (1) and E (2) in Taiwania cryptomerioides was achieved by combination of the photocyclization of 2, 3-dibenzylidenebutyrolactones (7 and 9) and subsequent air oxidation of the resulting β-apolignans (8a and 10a).View full abstractDownload PDF (607K) -
TAKASHI YATSUNAMI, SHUICHI FURUYA, TOSHIHIKO OKAMOTO1978 Volume 26 Issue 10 Pages 3199-3207
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAn aconite alkaloid, kobusine (1) was converted to a C14-C20 bond cleaved derivative (12) by a novel fragmentation reaction via a chloramine (11). Possible mechanisms were discussed in which participation of anionic nitrogen was proposed. The C14-C20 bond regeneration in compound (12) was also accomplished by an intramolecular Grignard type reaction.View full abstractDownload PDF (1115K) -
SHIGEO SENDA, KOSAKU HIROTA, TETSUJI ASAO1978 Volume 26 Issue 10 Pages 3208-3211
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS5, 6-Dicyano-1, 3-dimethyluracil (1) was synthesized stepwise from 6-chloro-5-formyl-1, 3-dimethyluracil (2). Treatment of 1 with butylamine or aniline afforded 6-butylamino-(5) or 6-anilino-5-cyano-1, 3-dimethyluracil (6), respectively. 3-Amino-5, 7-dimethylpyrazolo [3, 4-d] pyrimidine-4, 6 (5H, 7H)-dione (7) was obtained by the reaction of 1 with hydrazine hydrate. When 1 was refluxed in methanol in the presence of a catalytic amount of sodium methoxide, 5-cyano-6-methoxy-1, 3-dimethyluracil (9) was obtained. Acid hydrolysis of 1 afforded 6-carbamoyl-1, 3-dimethylorotic acid (10).View full abstractDownload PDF (614K) -
JUNICHI OHISHI, SHIRO IKEGAMI1978 Volume 26 Issue 10 Pages 3211-3214
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe p-nitrobenzoates of 2-methyltetrahydro-2-thiophenemethanol and 3-methyltetrahydro-3-thiopyranol have been synthesized. The rates of solvolysis of the esters in 80% aqueous acetone have been determined titrimetrically. The β-methyl substitution of the primary ester has caused the rate to increase by a factor of 28 and its rate is 3.9 times faster than that of the tertiary ester. Both esters yield the corresponding alcohols in similar ratio, so that it is concluded to intervene the same intermediary episulfonium ion.View full abstractDownload PDF (569K) -
MASASHI TOMODA, NORIKO SATOH, GO MATSUMURA1978 Volume 26 Issue 10 Pages 3215-3218
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe O-acetyl groups in paniculatan, the mucous polysaccharide isolated from the bark of Hydrangea paniculata SIEB., molecular weight of 545900, were located in position 3 of about 40% of L-rhamnopyranosyl residues. A completely deacetylated polysaccharide possessing significant lower molecular weight, 41950, was obtained by the action of 0.1 N sodium hydroxide at room temperature for 10 min, and the influence of this treatment on the partial degradation of a maoromolecule was considered.View full abstractDownload PDF (750K) -
TOZO FUJII, SHIGEYUKI YOSHIFUJI, MASASHI OHBA1978 Volume 26 Issue 10 Pages 3218-3222
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS3, 4-Dimethoxy, 3-benzyloxy-4-methoxy, 3, 4, 5-trimethoxy, 2-hydroxy-3, 4-dimethoxy, and 2-benzyloxy-3, 4-dimethoxy derivatives (3a-e) of phenacyl bromide have been prepared in 44-84% yields from the corresponding acetophenones by bromination with bromine in a mixture of ether and chloroform.View full abstractDownload PDF (747K) -
SUSUMU KITAGAWA, HISASHI TANAKA1978 Volume 26 Issue 10 Pages 3223-3225
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDimethylsulfoxide (DMSO) clathrates of some dithio metal complexes, bis (N-phenyl-β-mercaptothiocinnamamido) metal (II) bidimethylsulfoxide (ML2 (DMSO)2, M : Pt2+, Pd2+, Ni2+), bis {N-(2-methylphenyl)-and bis {N-(2, 6-dimethylphenyl)-β-mercaptothiocinnamamido} palladium (II) bidimethylsulfoxide (PdL'2 (DMSO)2 and PdL2" (DMSO)2, respectively) were prepared. From the results of infrared spectra and magnetic susceptibility measurements, these DMSO molecules were supposed to interact with the thioamido protons of the ligands by forming hydrogen bonds.View full abstractDownload PDF (435K) -
MITSUYA TANAKA, SHIGEHISA KYOSAKA, SANAE MURATA1978 Volume 26 Issue 10 Pages 3225-3228
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSBovine liver β-acetylhexosaminidase A (Hex A) and B (Hex B) were purified by hydrophobic affinity chromatography. Octyl Sepharose CL-4B was more effective than Phenyl Sepharose CL-4B as an adsorbent. Both the crude and the purified preparations of Hex A and Hex B exhibited extensive heterogeneity when focused on a polyacrylamide gel plate with pH gradient ; Hex A gave at least ten bands with pI's ranging from 5.0 to 7.0, and Hex B at least fourteen bands with pI's ranging from 6.5 to 8.5. Stepwise elution with increasing pH from a CM-cellulose column resulted in rough separation of Hex A and Hex B into overlapping classes.View full abstractDownload PDF (595K) -
HIDEO IIDA, SAKAE AOYAGI, KENSUKE KAWANO, CHIHIRO KIBAYASHI1978 Volume 26 Issue 10 Pages 3229-3233
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe reaction of the N-phenylacetyl and N-phenylpropionyl derivatives of 1, 2, 3, 3a, 4, 5-hexahydro-6H-indol-6-one (3 and 10) toward nucleophilic species are described. Several examples demonstrating intermolecular and intramolecular reactions occurring on the two electrophilic sites of the enamino ketone function and potential utility of these reactions on the synthesis of heterocyclic compounds are presented. A possible mechanism to rationalize these products is also presented.View full abstractDownload PDF (628K) -
TOZO FUJII, TAKASHI HIRAGA, SHIGEYUKI YOSHIFUJI, MASASHI OHBA, KIYOSHI ...1978 Volume 26 Issue 10 Pages 3233-3237
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS3-tert-Butylpyridine (11) has been synthesized from neopentyl alcohol in 16% overall yield through a five-step sequence. Among the steps involved are the cycloaddition of α-tert-butylacrolein (9) to butyl vinyl ether and conversion of the resulting dihydropyran derivative (10) into the pyridine base (11).View full abstractDownload PDF (761K) -
SADAO NISHIGAKI, YUKAKO KANAMORI, JUNKO SATO, KEITARO SENGA1978 Volume 26 Issue 10 Pages 3237-3239
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe reaction of 6-benzylidenehydrazino-1, 3-dimethyluracils with phosphorus oxychloride gave N4-benzylideneamino-6-chloro-1, 3-dimethylcytosines, which serve as useful substrates for several nucleophilic displacements.View full abstractDownload PDF (450K) -
KEITARO SENGA, YUKAKO KANAMORI, SADAO NISHIGAKI1978 Volume 26 Issue 10 Pages 3240-3241
Published: October 25, 1978
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTreatment of 6-substituted amino-5-benzylideneamino-1, 3-dimethyluracils with thionyl chloride at 0° for 30 min gave the corresponding 9-substituted 8-aryltheophyllines in 56-98% yields.View full abstractDownload PDF (353K)