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Volume 20, Issue 2
Displaying 1-38 of 38 articles from this issue
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YOSHIRO MIURA, HIROSHI SUGIYAMA, YUJI MAKI, SHUICHI SETO1972 Volume 20 Issue 2 Pages 215-218
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESS19-Tyrosine melittin, H-Gly-Jle-Gly-Ala-Val-Leu-Lys-Val-Leu-Thr-Thr-Gly-Leu-Pro-Ala-Leu-Ile-Ser-Tyr-Ile-Lys-Arg-Lys-Arg-Gln-Gln-NH2, was synthesized by the solid phase method using with the automatic instrument.It was obtained in 21% yield based on the amount of gultamine initially esterified to the resin.The hemolytic activity of that compound was examined.View full abstractDownload PDF (755K) -
HIKOKICHI OURA, KINJI TSUKADA, HITOMI NAKAGAWA1972 Volume 20 Issue 2 Pages 219-225
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSIt was shown that a single intraperitoneal injection of extract (fraction 4) from roots Panax ginseng C.A.Meyer, increased the incorporation rate of labeled precursor into cytoplasmic polysomal ribonucleic acid (RNA) of rat liver.The content of heavy poly-somes (over hexamer) in postmitochondrial supernatant from liver treated with fraction 4 was observed to increase at 6 and 10 hr after treatment.Sedimentation analysis of ribosomal RNA and messenger RNA derived from polysomes showed that the newly induced RNA by fraction 4 is evenly distributed over all RNA. Particularly, 29S ribosomal and 9-10S messenger RNAs were stimulated significantly. In an amino acid incorporation system in vitro, stimulatory activities of microsomes and polysomes from treated rat liver are more active by 85 and 67% than those from normal liver, respectively.View full abstractDownload PDF (1045K) -
HIROSHI HONGO1972 Volume 20 Issue 2 Pages 226-231
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSIn the previous paper, it was reported that the structure of the adduct (II), which was produced from the Diets-Alder reaction of 1-methyl-2-(1H) pyridone (I) with maleic anhydride, was estimated to be 2-methyl-3-oxo-2-azabicyclo [2.2.2] oct-7-ene-5, 6-endo-dicarboxylic anhydride. It was also mentioned that the structure of the diester com-pound (IV), which was obtained by the epimerization, was estimated to be dimethyl 2-methyl-3-oxo-2-azabicyclo [2.2.2] oct-7-ene-5-endo-6-exo-dicarboxylate.
In this work, the same reactions were carried out on 3, 5-dideutero-1-methyl-2 (1H)-pyridone (ID). The structures of II and IV were unambiguously confirmed to the same as those in the previous paper.View full abstractDownload PDF (772K) -
MASAMI INOUE, SABURO ENOMOTO1972 Volume 20 Issue 2 Pages 232-237
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSThe alkylation of phenol by C1-C3 alcohols as alkylating reagents was examined on alumina and alumina containing catalysts. Alumina showed a significant activity to meta position, especially in methylation and ethylation. For instance, the composition of meta isomer was 38% in cresols formed at 450°. Alumina-silica (1: 1) yielded 48% meta isomer. The latter catalyst was an acidic one, and the formation of meta isomerin parallel with its acid strength.
To elucidate the mechanism of alkylation to meta position, the rearrangement of-phenylethers and the isomerization of ortho alkylphenols were investigated in the presence of phenol-14C. The 14C-distribution in the product was then determined by the radio-gaschromatography and the ratio of intramolecular to intermolecular rearrangement was evaluated. The adsorbed state of phenol and alcohols at the reaction temperature was investigated with the infrared method, and the mechanism of alkylation was discus-sed therefrom.View full abstractDownload PDF (877K) -
TSUNEYOSHI YAMAZAKI, TADASHI OOHAMA, TORU DOIUCHI, TAKEO TAKIZAWA1972 Volume 20 Issue 2 Pages 238-245
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSCyclopenten-3, 4, 5-triones having phenyl, methoxy, and dialkylamino groups at their olefinic double bonds were synthesized, and their structural properties were discussed from their infrared and ultraviolet spectra, and pk values. It is proposed that delocali-zability of electron system of the ring is greatly affected by the electron donating ability of the substituent, and that the ring system having strong electron donating groups has a kind of aromaticity.View full abstractDownload PDF (1339K) -
KUNIO HIROI, KAZUO ACHIWA, SHUN-ICHI YAMADA1972 Volume 20 Issue 2 Pages 246-257
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSThis paper is concerned with the asymmetric synthesis of 2-alkylcyclohexanones (VI) by alkylation of cyclohexanone enamines (III) of L-proline ester derivatives. Acrylonitrile, methyl acrylate, allyl bromide and ethyl bromoacetate were used as alkylating agents. Several reaction conditions were examined, and plausible reaction mechanisms were proposed. Rates of racemization for VIa and -Vic were determined.View full abstractDownload PDF (2015K) -
IKUO MORIGUCHI, SHIZUO FUSHIMI, NOBUYOSHI KANENIWA1972 Volume 20 Issue 2 Pages 258-261
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSThe effects of water on charge-transfer (CT) transition energy, hνCT, and the equilibrium constant, Kc, for complexations of chlorpromazine hydrochloride with p-xyloquinone and sodium N, N-dimethyl-p-aminobenzoate with sodium anthraquinone-2-sulfonate were investigated in aqueous ethanol, aqueous dioxane, or water. With an increase water content of the media, hνCT decreased and Kc increased markedly. Especially correlations were recognized between hνCT and water content, and between log Kc logarithm of dielectric constant of the media. From the results, mechanism of the of water was speculated. It may be concluded that water does not obstruct but promotes the CT complexations presumably by specific and non-specific effects.View full abstractDownload PDF (531K) -
SHOSUKE KAWANISHI, AKIRA YOKOYAMA, HISASHI TANAKA1972 Volume 20 Issue 2 Pages 262-268
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSInfrared and nuclear magnetic resonance spectra of palladium (II) monothio-β-diketonates were studied in comparison with those of palladium (II)β-diketonates. The following novel reactions have been found. Namely, palladium dithioacetylacetonate was obtained in the reaction of monothioacetylacetone and palladium ion in acid solution by the reaction which may be called as “ligand atom replacement reaction” and palladium monothio-β-diketonates were obtained from disulfides of monothio-β-diketones and palladium ion. The reason for the occurance of this reaction may be reasonably explained by the high affinity between palladium and sulfur and the high stability of the palladium chelates formed.View full abstractDownload PDF (844K) -
TAKASHI TSUCHIYA, HEIHACHIRO ARAI, HIROYUKI KAWAMURA, HIROSHI IGETA1972 Volume 20 Issue 2 Pages 269-272
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSPhotolysis of 3-hydroxy-6-phenylpyridazine (III) in CH3OH containing 5% HCl, afforded methyl 3-benzoylpropanoate (V) and methyl 2-methyl-3-benzoylpropanoate (VI), and three kinds of nitrogen free compounds. Similarly, 3-chloro-6-phenylpyridazine (IV) afforded V, methylated pyridazines (VII, VIII, IX, X, and XI), hydroxymethylated pyridazine (XI), and small amounts of nitrogen free compounds.View full abstractDownload PDF (526K) -
TAKASHI TSUCHIYA, HEIHACHIRO ARAI, HIROSHI IGETA1972 Volume 20 Issue 2 Pages 273-276
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSIrradiation of Pyridazine (Ia) in methanol containing 5% HC1, afforded 4-methylated and 4, 5-dimethylated compounds. 3-Methylpyridazine (Ib) gave 4-methylated compound, along with 5-methylated and 4, 5-dimethylated compounds. 3-Methoxypyridazine (Ic) afforded 4-methylated and 4, 6-dimethylated compounds. 3, 6-Dimethylpyridazine (Ie) gave 4-methylated and 4, 5-dimethylated compounds. 3-Methoxy-6-methylpyridazine (If) gave 4-methylated compound as a sole product. 3-Methyl-6-chloropyridazine (Ig), 3, 6-dichloropyridazine (Ih), and 3-phenyl-6-chloropyridazine (Ii) afforded 5-methylated and 4, 5-dimethylated compounds, respectively. 3-Chloropyridazine (Id) did not give monomethylated, but 4, 5-dimethylated compound in a low yield. of 1-2%, presumably due to the unstability and the decomposition of the starting material.View full abstractDownload PDF (435K) -
SHIOTANI SHIOTANI, KOMETANI TADASHI, MITSUHASHI KEMMOTSU1972 Volume 20 Issue 2 Pages 277-283
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSSynthetic routes of 3-methyl-2, 3, 4, 5, 6, 7-hexahydro-2, 7-methano-1H-3-benzazonine (X-A), 4-methyl-2, 3, 4, 5, 6, 7-hexahydro-1, 6-methano-1H-4-benzazonine (X-B) and 2-methyl-2, 3, 4, 5, 6, 7-hexahydro-1, 6-methano-1H-2-benzazonine (XX) having a new ring system were described.
4-Phenylcyclohexanone (I) was condensed with diethyl oxalate followed by decarbonylation to give ethyl 2-oxo-5-phenylcyclohexanecarboxylate (II), which was hydrolyzed to afford 4-phenylpimelic acid (III). 5, 9-Methanobenzocycloocten-8, 10-dione (IV) obtained by cyclization of III with PPA was reduced to 10-hydroxy-5, 9-methanobenzocycloocten-8- one (V), which in turn was derived to 8-acetoxy-5, 9- methanobenzocyclooctene (VI) by catalytic reduction over Adams catalyst in acetic acid containing a small amount of perchloric acid. VI was hydrolyzed, followed by a Jones oxidation to give 5, 9-methanobenzocycloocten-8-one (VII). The oxime (VIII) of VII was submitted to a Beckmann rearrangement with PPA to afford a mixture of 2, 3, 6, 7-tetrahydro-2, 7-methano-1H-3-benzazonin-4 (5H)-one (IX-A) and 2, 3, 6, 7-tetrahydro-1, 6-methano-1H-4-benzazonin-5 (4H)-one (I X -B)(ratio: ca. 10: 1), which were separated by fractional recrystallization. Both IX-A and IX-B were reduced with lithium aluminum hydride, followed by Clarke-Eschweiler methylation to give X-A and X-B, respectively.
4-Benzylcyclohexanone (XIV) obtained by catalytic reduction of p-benzylphenol (XIII) and the subsequent oxidation with chromic acid was derived to 3-benzyladipic acid (XV) by nitric acid oxidation, which was then cyclized to 4-oxo-1, 2, 3, 4-tetrahydronaphthalene-2-propionic acid (XVI). The ethyl ester (XVII) of XVI was derived to the oxime (XVIII), which was reduced to an amino-ester followed by cyclization to give 4, 5, 6, 7-tetrahydro-1, 6- methano-1H-2-benzazonin-3 (2H) one (XIX). Reduction of XIX with lithium aluminum hydride and the subsequent methylation afforded XX.View full abstractDownload PDF (1169K) -
ISAO MATSUNAGA, ZENZO TAMURA1972 Volume 20 Issue 2 Pages 284-286
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSA simple and reliable analytical method for D-glucaric acid, D-glucaro-1, 4-lactone and-6, 3-lactone was established; the sample solution was freeze-dried, trimethylsilylated and applied to a gas chromatograph.
The transformation of D-glucaro-1, 4-lactone into D-glucaric acid and D-glucaro-6, 3-lactone at physiological pH and temperature was traced by this method. Similarly, the transformations of L-gulono-γ-lactone into L-gulonic acid and of D-glucono-γ-lactone into D-gluconic acid and D-glucono-δ-lactone were traced.View full abstractDownload PDF (323K) -
TOSHIO NAMBARA, HIROSHI HOSODA, TAKAKO ANJYO, MARIKO YAMAUCHI, JUNKO M ...1972 Volume 20 Issue 2 Pages 287-294
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSIn order to clarify the stereochemistry of hydrogen loss from C-2 in the 19-norsteroid during the placental aromatization the stereoselective synthesis of C-2 epimeric 2-deuterioestr-4-ene-3, 17-diones has been carried out. A key intermediate leading to the desired compounds, estr-2-ene-5βA, 17β-diol (VIII), was prepared from readily available 19-nortestosterone in several steps. Epoxidation with per-acid followed by trans-diaxial opening of the resulting 2βA, 3βA-epoxide (IX) with lithium aluminum deuteride provided the 2α-deuterio-3β, 5β, 17β-triol (XVII). On the other hand VIII was transformed into the 2β-deuterio-3βA, 5βA, 17βA-triol (XX) by treatment with deuterated diborane. Upon dehydration with thionyl chloride and subsequent oxidation with chromium trioxide-pyridine complex XVII and XX were led to 2-deuterated estr-4-ene-3, 17-diones (XIX, XXII), respectively.View full abstractDownload PDF (1407K) -
TETSUJI KAMETANI, MASUO KOIZUMI, CHIZUKO SEINO, TAKUO NAKANO1972 Volume 20 Issue 2 Pages 295-299
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSPhotolysis of the diazonium salt of 1-(2-amino-3-benzyloxy-4-methoxyphenethyl)-1, 2, 3, 4-tetrahydro-6, 7-dimethoxy-2-methylisoquinoline (VIIIa) gave O-benzylhomosalutaridine (VIIa).View full abstractDownload PDF (732K) -
TAKASHI TSUCHIYA, HEIHACHIRO ARAI, TATSUO TONAMI, HIROSHI IGETA1972 Volume 20 Issue 2 Pages 300-303
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESS3, 4, 5, 6-Tetraphenylpyridazine 1-oxide (II) was irradiated in acetone or dichloromethane with high pressure mercury lamp (200W) for 3 hr, affording tetraphenylfuran (III), dibenzoylstilbenes (IV and V), 1-(1, 2, 3-triphenylcyclopropeny1)-Δ3, 6-bicyclo [3, 2, 0]-heptadien-2-one (VI), and the deoxygenated starting material (I). 3, 4, 6-Triphenylpyridazine 1-oxide (VIII) gave triphenylfuran (IX), cis-dibenzoylstyrene (X), 3-benzoyl-1, 2-diphenyl-1-cyclopropene (XI), and the deoxygenated starting material (VII). The reaction mechanism is also discussedView full abstractDownload PDF (598K) -
KENTARO HIRAI, TERUYUKI ISHIBA1972 Volume 20 Issue 2 Pages 304-308
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSNovel S, O, N-triheterocation, N-(1, 3-oxathiol-2-ylidene) ternary iminium ion (II), was synthesized by cyclization of phenacyl l-piperidinecarbothiolate with concentrated sulfuric acid. A number of derivatives having various substituents at para position of 5-phenyl group in II were prepared. Physicochemical properties examined in these salts revealed that the immonium structure is more substantial than the 1, 3-oxathiolium structure.View full abstractDownload PDF (625K) -
AKIRA HARA, MINORU SEKIYA1972 Volume 20 Issue 2 Pages 309-313
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSTreatments of β-chlorovinylaldehydes with zinc powder in ethanol selectively remove the β-chlorine atom to give the α, β-unsaturated aldehydes. However, the same treatments in nitrogen atmosphere and, preferably, by using the activated zinc powder lowered remark ably the yield of the α, β-unsaturated aldehydes and give the reductive dimer, 1, 2-di-(1-alkenyl) ethylene glycol, as major product.View full abstractDownload PDF (769K) -
KEN'ICHI TAKEDA, SADAO YAMAMOTO1972 Volume 20 Issue 2 Pages 314-324
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSVarious stereoisomers of 6-substituted-trans-2-decalols have been synthesized; four possible epimers for 6-methoxy and 6-chloro derivatives, three epimers for 6-cyano derivatives, and two epimers for 6-phenyl, 6-carbomethoxy, and 6-oxo derivatives were reported. The structures of these compounds were assigned by proton magnetic resonance and infrared spectroscopies. A paramagnetic shift reagent, tris (dipivalomethanato) europium (III), was successfully applied in the proton magnetic resonance spectra of the two epimers of trans-2-decalol to establish their structures.The spectral data obtained were also presented and discussed.View full abstractDownload PDF (3332K) -
YOSHIO ARATA, TOYOHIKO KOBAYASHI1972 Volume 20 Issue 2 Pages 325-329
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSReaction of Δ1, 10-hexahydroquinolizine (I) with trichloroacetic acid in benzene afforded 6-chloro-1-azabicyclo [4.4.1] undecan-11-one (II). Acid hydrolysis of II followed by hydrogenation on palladium-charcoal yielded 6-carboxydecahydroazecine (IV), and alkali hydrolysis of II followed by lithium aluminum hydride reduction gave 10-hydroxymethyl-octahydroquinolizine (IX), which was also obtained by lithium aluminum hydride reduction of II. Reaction of II with sodium in liquid ammonia gave both 1-azabicyclo-[4.4.1] undecan-11-ol (XIII) and 6-carbamoyldecahydroazecine (XIV). The action of p-toluenesulfonyl chloride on the latter compound, followed by reduction with lithium aluminum hydride afforded 1-azabicyclo [4.4.1] undecane (XVI).View full abstractDownload PDF (941K) -
TOSHIO MIYAZAKI, TSUTOMU IRINO1972 Volume 20 Issue 2 Pages 330-335
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSThe main polysaccharide of A. cylindrospora, [α] D+15.0°, in a highly complicated heteroglycan composed of fucose, mannose, glucose, galactose, N-acetylglucosamine, and N-acetylgalactosamine in a relative ratio of 10: 25: 4: 2: 2: 1 and that of M. mucedo, [α] D+30.4°, contains the same componental sugars in a molar ratio of 10: 25: 2.1: 3.6: 4: 2. The results of periodate oxidation and partial acid hydrolysis of both polysaccharides indicate a similarity in their structural feature.
The minor polysaccharide of A. cylindrospora, [α] D+43.6°, has the same componental sugars as the main polysaccharide but that of M. mucedo, [α] D-65.0°, is an acidic heteroglycan consisting of fucose, galactose, and glucuronic acid.View full abstractDownload PDF (1039K) -
TOSHIO NAMBARA, KAZUTAKE SHIMADA, YOUICHI FUJII, MOTOHIKO KATO1972 Volume 20 Issue 2 Pages 336-342
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSThe synthesis of 1, 2- and 2, 3-dimethoxy-4-methylestra-1, 3, 5 (10)-trien-17β-ols (XIIIc, VIII c) from androsta-1, 4-diene-3, 17-dione (I), which is readily available as the micro-bial transformation product derived from cholesterol, has been undertaken. The desired compounds could be obtained by introducing an oxygen function into 1-and 3-methoxy- 4-methylestratrienes (XIc, VId) employing Friedel-Crafts reaction with acetyl chloride followed by Baeyer-Villiger oxidation as shown in Chart 1 and 2.View full abstractDownload PDF (1204K) -
MINORU SEKIYA, KUNIO SUZUKI1972 Volume 20 Issue 2 Pages 343-348
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSReductive fission of one of the carbon-carbon bonds of the alkylidene- or aryl-methyl-ene-bond bridged between the two active carbons has been generalized in several examples by means of heating with the formate, triethylammonium formate which has been known as a distil lable liquid given by 5HCO2H·2NEt3.View full abstractDownload PDF (1067K) -
TATSUJI IGA, SHOJI AWAZU, HISASHI NOGAMI1972 Volume 20 Issue 2 Pages 349-356
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSThe relationship between the biliary excretion behavior and the elimination from plasma was studied using five xanthene dyes, i.e. Phloxine B (PB), Rose Bengal (RB), Erythrosine B (EB), Eosine Y (EY) and Fluorescein sodium (FS), and Bromsulphthalein (BSP) in vivo and in vitro in rat.
1) It was of interest that the plasma elimination patterns of xanthene dyes showed two types, the elimination following the one and two compartments models. PB and RB were the former group, and EB, EY and FS were the latter group.
2) The plasma elimination of xanthene dyes except for FS which has no halogen substituent, were relatively rapid (T1/2=3-12min). But the elimination of FS was very slow (T1/2=60min), and it was suggested that the effect of the halogen substituent was shown in the plasma elimination as well as in the biliary excretion.
3) The binding ratio with rat plasma of xanthene dyes showed similar ratios (55-70%) with each other except for FS. The ratio of FS was very low (15%) in spite of it's slow plasma elimination.
4) The plasma elimination of BSP was very rapid (T1/2=3.3min) and followed the two compartment model, but the binding ratio with plasma protein was rather high (about 50%) in spite of its rapid plasma elimination and concentrical biliary excretion.
5) It was also found that the bile acid gave some influence on the binding with BSA.View full abstractDownload PDF (931K) -
SADAO UCHIYAMA, HIROYA TANABE, ZENZO TAMURA1972 Volume 20 Issue 2 Pages 357-360
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSFrom the reaction of dulcin and sodium nitrite, a fluorescent compound (colorless crystals, mp 183-184°) was obtained. The structure of this fluorescent compound was presumed to be 1, 3-bis (4-ethoxypheny1)-5-tetrazolone by nuclear magnetic resonance, infrared, mass spectroscopy and by several reactions.View full abstractDownload PDF (440K) -
HIDEO SEKI, KENJI KOGA, SHUN-ICHI YAMADA1972 Volume 20 Issue 2 Pages 361-367
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSMixed carbonic-carboxylic acid anhydrides prepared from N-acylated a-amino acids and ethyl chloroformate in tetrahvdrofuran were reduced to the corresponding N-acylated a-amino aldehydes with palladium-charcoal under hydrogen bubbling. The optimum conditions found for N-acetyl-L-alanine were applied to the conversion of several kinds of N-acylated x-amino acids to their corresponding aldehydes, as shown in Table II. It was found that considerable racemization occurred under the present reduction conditions.
Oxidation of some N-acylated β-amino alcohols with dimethylsulfoxide in the presence of dicyclohexylcarbodiimide and phosphoric acid was also studied.View full abstractDownload PDF (1226K) -
EIICHI FUJITA, AKIHISA SUMI, YOKO YOSHIMURA1972 Volume 20 Issue 2 Pages 368-379
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSOptically active O-methylthalicberine, a major bisbenzylisoquinoline-type alkaloid of Thalictrum Thunbergii DC., was synthesized through a number of steps of reactions shown in Charts 4 to 7. A preliminary confirmation of its structure has also been described.View full abstractDownload PDF (1859K) -
Accès aux Furoacridines par Application de la Réaction de FriedlaenderKANAME TAKAGI, TAKEO UEDA1972 Volume 20 Issue 2 Pages 380-384
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSLes méthyl-2-, phényl-2- et p-méthoxyphényl-2 oxo-4 tétrahydro-4, 5, 6, 7 benzofurannes peuvent se condenser sur 1' amino-2 acétophénone, 1'amino-2 benzophénone et le benzoyl-1 amino-2 naphtalène pour former de nouveaux dérivés de la dihydro-furoacridine. L'emploi des chlorhydrates des composés o-aminophényl carbonylés, au lieu des amines libres, favorisent notablement cette réaction. Certains des composés originaux obtenus peuvent être déhydrogénes en furoacridines par le charbon palladié.View full abstractDownload PDF (675K) -
SHOSHIRO NAKAMURA, HIDEO FUKUDA, TAKUZO YAMAMOTO, MICHIKO OGURA, MASA ...1972 Volume 20 Issue 2 Pages 385-390
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSAlkaline proteinases, named alkinonase A and AF, are isolated from the cultured broth of Streptomyces violaceorectus. Both alkinonases show remarkably strong antiinflammatory activity for the carrageenin-induced edema. Alkinonase A and AF are belonging to a new type of alkaline proteinases of microbial origin. The effect of inhibitors on the proteolytic activity and the substrate specifities of alkinonases are resembled to that of the neutral proteinases of microbial origin and different from that of the alkaline proteinases of microbial origin. Production, isolation, purification, effect of pH on the proteolytic activity, pH stability, effect of temperature on the proteolytic activity, effect of inhibitors on the proteolytic activity, substrate specifities and anti-inflammatory activity for the carrageenin induced edema of alkinonases are described in this paper.View full abstractDownload PDF (752K) -
SHIGEO SENDA, KOSAKU IROTA, GUANG-NAN YANG1972 Volume 20 Issue 2 Pages 391-398
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSAn alkylation of 3-amino-4-ethoxycarbonylpyrazole (1) under various conditions was investigated. Alkylated pyrazoles (2, 3a, b) were condensed with isocyanates or isothiocyanate to yield pyrazolylurea derivatives (4a-f, 10). Ring closure of these intermediates was carried out in a solution of sodium ethoxide and the resulting 2, 5 (or 1, 5)-disubstituted pyrazolo [3, 4-d] pyrimidines (5a-f, 11a, b) were alkylated to give 2, 5, 7 (or 1, 5, 7)-trisubstituted pyrazolo [3, 4-d] pyrimidines (6a-e, 12a, b) or 2, 5-disubstituted 6-methylmercaptopyrazolo [3, 4-d] pyrimidines (7a, b). Instead of the use of isocyanates, another methods by fusing ureas with methylpyrazole were also investigated. Furthermore, debenzylation of 2-benzylpyrazolo [3, 4-d] pyrimidines (6c, d) was carried out with 35 atm of hydrogen in an autoclave at 220°over palladium on carbon to give debenzylated compounds (13a, b).View full abstractDownload PDF (1129K) -
SENDA SHIGEO, HIROTA KOSAKU, YANG GUANG-NA1972 Volume 20 Issue 2 Pages 399-403
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSReactions of 1, 3-disubstituted 6-chloro-5-formyluracils (1) with phenylhydrazine or methylhydrazine giving 1, 5, 7-and 2, 5, 7-trisubstituted 4, 6-dioxo-4, 5, 6, 7-tetrahydropyrazolo [3, 4-d] pyrimidines (3, 7 and 4) were investigated in detail. It was found out that 5-formyl group in 1 was more reactive than that 6-chloro group. Thus, under cold condition, the reaction of 1 with phenylhydrazine yielded Schiff's bases (2). Upon heating, 1 with equimolar or two equivalent moles of phenylhydrazine gave isomeric compounds, 3 and 4, which were also prepared by other routes. Reactions of methylhydrazine with 1 were also investigated. Furthermore, the Schiff's bases were made to react with other kinds of hydrazines. The reaction products showed that substituent at 1- or 2-position of the products (4, 7) depended on the kind of hydrazine used later.View full abstractDownload PDF (829K) -
HARUO OGURA, MASAKAZU SAKAGUCHI, KAZUYOSHI TAKEDA1972 Volume 20 Issue 2 Pages 404-408
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESS7-Substituted 1, 3-dimethyl-7H-2, 4, 6-(5H, 6H) pyrrolo [2, 3-d] pyrimidinetriones (IIIa, b, c) were prepared from 6-amino-1, 3-dimethyluracil (I) and ethyl α-bromoacetate. Reactionof I and α-bromo-ketones afforded 6, 7-disubstituted 1, 3-dimethyl-7H-2, 4-pyrrolo-[2, 3-d] pyrimidinediones (IV, V, VI). On the other hand, reaction of 6-mercapto-1, 3-dimethyluracil (VIII) and cc-bromocarbonyl compound afforded thieno [2, 3-d] pyrimidines (X, XI).View full abstractDownload PDF (622K) -
TAKAKO INOUE, YUJI NAKAHARA, TETSUKICHI NIWAGUCHI1972 Volume 20 Issue 2 Pages 409-411
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
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IKUO MORIGUCHI, SHIZUO FUSHIMI, NOBUYOSHI KANENIWA1972 Volume 20 Issue 2 Pages 411-414
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSCharge-transfer (CT) is known to take part in various complexations and reactions. Because the most phenomena of pharmaceutical interest occur in aqueous media, the effect of water on CT has become an important subject in the pharmaceutical field. The previous study has demonstrated that water promotes the formation of outer complexes. In the present study, attention has been drawn to the rate of CT reaction. As the example in this work, aniline-chloranil system has been taken on which detailed studies carried out with respect to the outer complex formation and the CT reaction.View full abstractDownload PDF (430K) -
YOSHINORI KIDANI, MASAHIDE NOJI, HISASHI KOIKE1972 Volume 20 Issue 2 Pages 415-417
Published: February 25, 1972
Released on J-STAGE: May 27, 2011
JOURNAL FREE ACCESSSince some of oxine-like compounds showed antibacterial action in the presence of certain metal ions, this experiment was carried out to synthesize a model compound of mixed-ligand complexes of 8-hydroxyquinoline-5-sulfonic acid (abbr. as HQS below), being a water soluble oxine derivative, L-histidine (abbr. as His) and certain metal ions. The authors reported on the synthesis of the mixed-ligand complex of Co (III) containing oxine and glycine. In this paper His was used as a chelating amino acid, which is expected to form mixed-ligand complexes more easily than in the case of glycine in cooperating with HQS, since the stability constants of His-metal complexes are much closer to those of HQS-metal complexes.View full abstractDownload PDF (390K) -
TOSHIHIKO OKAMOTO, MITSUTAKA NATSUME, TADAMASA ONAKA, FUMIHIKO UCHIMAR ...1972 Volume 20 Issue 2 Pages 418-421
Published: February 25, 1972
Released on J-STAGE: January 31, 2011
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HIROSHI HIKINO, SHINJI KORIYAMA, TOMIHISA OHTA, TSUNEMATSU TAKEMOTO1972 Volume 20 Issue 2 Pages 422-423
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
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JUNZO SHOJI, YASUMASA TSUKITANI1972 Volume 20 Issue 2 Pages 424-426
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
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KUNITOSHI YOSHIHIRA, MASAMICHI FUKUOKA, MASANORI KUROYANAGI, SHINSAKU ...1972 Volume 20 Issue 2 Pages 426-428
Published: February 25, 1972
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSDownload PDF (358K)
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