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Volume 25, Issue 2
Displaying 1-31 of 31 articles from this issue
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TETSUZO KATO, TAKUO CHIBA, HITOSHI KIMURA1977 Volume 25 Issue 2 Pages 203-208
Published: February 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSReaction of 4-bromoacetoacetanilide (II) with pyridine (Ia), 4-methylpyridine (Ib), and 3-methylpyridine (Ic) gave pyridinium (IVa), 4-methylpyridinium (IVb), and 3-methylpyridinium (N-phenylcarbamoyl) acetonylide (IVc), respectively. These ylides (IVa, b, c) were allowed to react with diethyl acetylenedicarboxylate (DEAC) to give diethyl 3-(N-phenylcarbamoyl) acetylpyrrolo [1, 2-a] pyridine-1, 2-dicarboxylate (VIa), and its methyl derivatives (VIb, VIc, and VId). Reaction of ethyl 4-bromoacetoacetate (III) with pyridines (Ia, b, c) followed by treatment with DEAC afforded the pyrrolo [1, 2-a] pyridine derivatives (VIIa, b, c, d). Similarly, quinoline (VIIIa) and 4-methylquinoline (VIIIb) reacted with II (III) to give the corresponding N-ylides, IXa and IXb (Xa and Xb), respectively. These ylides were converted to the pyrrolo [1, 2-a] quinoline derivatives (XIa, b and XIIa, b). Similar reaction of isoquinoline gave the pyrroloisoquinoline derivatives (XIII, XIV).View full abstractDownload PDF (831K) -
JUN OKUDA, YUJI TSUZUKI1977 Volume 25 Issue 2 Pages 209-214
Published: February 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSMethylmercuric chloride (MMC, CH3HgCl) was adminsitered to male Wistar rats weighing 150-160 g by subcutaneous injection in a daily dose of 1 mg or 0.4 mg per 100 g body weight to produce an acute (for 12 days, 20 rats) or a subacute intoxication (for 28 days, 20 rats). Hematocrit value decreased from 37% (control group) to 27% (MMC administered groups) with decreasing body weight. About 90% of total mercury in the blood (ca. 95μg Hg/ml) of rats of the two MMC-treated groups was distributed in the erythrocytes. The shapes of erythrocytes (acute and subacute intoxications) became the spicule cells like acanthocyte. The osmotic fragility of erythrocytes of rats with acute intoxication clearly decreased, but oxygen capacity per ml of the erythrocytes did not change. Then, the properties of the erythrocytes incubated with various concentrations (44, 72, 170 μg Hg/ml) of MMC for 60 min at 37°were studied. Spicule cells like echinocyte II increased with increasing mercury amount into erythrocytes. However, the osmotic fragility and oxygen capacity per ml of the erythrocytes were unchanged.View full abstractDownload PDF (1115K) -
TETSUO KATO, NORIICHI ODA, ISOO ITO1977 Volume 25 Issue 2 Pages 215-220
Published: February 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe conversion of 2, 4-dialkoxypyrimidines into 1, 3-dialkyl-1, 2, 3, 4-tetrahydro-2, 4-dioxopyrimidines was brought about in the presence of p-toluenesulfonic acid derivatives by simple heating. This reaction seems to proceed stabilized transition state in p-toluenesulfonic acid derivatives, and may give rise to a nucleophilic reaction by nitrogen on the migrating alkyl group.View full abstractDownload PDF (680K) -
YASUMASA HAMADA, TAKAYUKI SHIOIRI, SHUNICHI YAMADA1977 Volume 25 Issue 2 Pages 221-223
Published: February 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe synthesis of the N-terminal hexapeptide of the vasoactive intestinal peptide (VIP), His-Ser-Asp-Ala-Val-Phe (II) was carried out by the both fragment condensation and stepwise elongation approaches using mainly diphenyl phosphorazidate (DPPA) as a coupling reagent.View full abstractDownload PDF (555K) -
YASUMASA HAMADA, SUSHMA RISHI, TAKAYUKI SHIOIRI, SHUNICHI YAMADA1977 Volume 25 Issue 2 Pages 224-230
Published: February 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe synthesis of the N-terminal decapeptide of gastric inhibitory polypeptide (GIP), Tyr-Ala-Glu-Gly-Thr-Phe-Ile-Ser-Asp-Tyr (IV), was carried out in two ways (F1+F2-4+F5-10 and F1-4+F5-10) using diphenyl phosphorazidate (DPPA) and diethyl phosphorocyanidate (DEPC) as coupling reagents.View full abstractDownload PDF (984K) -
NAOKI MITSUO, TAKEHISA KUNIEDA, TAKEO TAKIZAWA1977 Volume 25 Issue 2 Pages 231-238
Published: February 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSmooth conversion of telomers of vinylene carbonate with carbon tetrachloride or methylene bromide as a telogen to novel trans enol phosphates, and the reactivities of the phosphates thus formed are described. Both trans-"anti"-trans- and trans-"syn"-trans-isomers of the n=2 telomers, 5-chloro-5'-trichloromethyl-(4, 4'-bi-1, 3-dioxolan)-2, 2'-dione and 5-bromo-5'-dibromomethyl-(4, 4'-bi-1, 3-dioxolan)-2, 2'-dione gave, on treatment with trialkyl phosphites, the identical trans dialkyl 2-(5-trichloromethyl- and 2-(5-dibromomethyl-2-oxo-1, 3-dioxolan-4-yl) vinyl phosphates in good yields, without any detectable amount of cis isomer and the phosphonate, while the n=1 adduct failed to give the corresponding enol phosphate. Stereospecific conversion of the phosphate to cis 2-(5-trichloromethyl-2-oxo-1, 3-dioxolan-4-yl) vinyl acetate was readily achieved by new vinylic exchange reaction catalyzed by palladium chloride in acetic acid by way of the processes, trans oxypalladation and trans deoxypalladation. Reactions involving catalytic hydrogenation, chlorination with titanium chloride and conversion to α, β-unsaturated aldehydes are summarized in Chart 2.View full abstractDownload PDF (912K) -
TSUTOMU MATSUURA, TAKEHISA KUNIEDA, TAKEO TAKIZAWA1977 Volume 25 Issue 2 Pages 239-245
Published: February 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFacile routes to trichloromethyl-containing aldoses and polyalcohols from low telomers of vinylenecarbonate with carbon tetrachloride are described. 3, 3, 3-Trichloro-3-deoxyglyceraldehyde derived from n=1 adduct was dimerized to five-membered 1, 3-dioxolane derivative preferentially, in contrast to the corresponding 3, 3-dichloro compound which gave the dimer in 1, 4-dioxane structure. Three-step procedure involving acetalization followed by removal of cyclic carbonate groups and subsequent deacetalization was mild and selective enough to permit the hydrolysis of n=2 telomers to 5, 5, 5-trichloro-5-dioxy-DL-lyxose and -xylose in excellent yields, while acid hydrolysis under more drastic conditions (at 100-110°) gave the rearranged 5, 5, 5-trichloro-3, 5-dideoxy-pentosulose in dimeric form exclusively. Reduction of telomers (n=1 and 2) and the derivatives with sodium borohydride gave polyalcohols of the type Cl3C-(CHOH)n-H (n=2, 3, and 4), among which some compounds showed considerable sedative activities.View full abstractDownload PDF (899K) -
KATSUMI MIYAZAKI, OSAMU OGINO, MASAHIRO NAKANO, TAKAICHI ARITA1977 Volume 25 Issue 2 Pages 246-252
Published: February 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn order to investigate the reasons why the body fluid concentrations of pivampicillin and amoxicillin were higher than those of ampicillin after administration of the drugs to rats and humans, the mechanisms of intestinal absorption of these antibiotics in rats were examined using the new fluorometric determination method. In these experiments, it was found that the higher lipid solubility and the greater dissolution rate of pivampicillin are the main reasons for the higher body fluid concentrations of ampicillin after administration of pivampicillin. However, the higher body fluid concentrations of amoxicillin could not be explained on the basis of these physicochemical properties. In the studies using the rat small intestinal segments, i.e. the everted intestine, everted sac and the intact intestinal loop, greater binding to the mucosa of amoxicillin than of ampicillin was observed. This observation may provide an explanation for the difference in body fluid concentrations of these two drugs. These two amphoteric penicillins may be absorbed from the rat small intestine by passive diffusion mechanism.View full abstractDownload PDF (797K) -
KATSUMI MIYAZAKI, OSAMU OGINO, HIROYUKI SATO, MASAHIRO NAKANO, TAKAICH ...1977 Volume 25 Issue 2 Pages 253-258
Published: February 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn order to estimate the transfer of amoxicillin in the body fluids, a direct separatory determination method of amoxicillin and its penicilloic acid was investigated. The penicilloic acid of amoxicillin formed an intensive and reproducible fluorescent product in solutions containing mercuric chloride, but the fluorescent product was not formed from amoxicillin directly. From these observations, the measurement can be made of amoxicillin and its penicilloic acid separately in urine and blood following therapeutic doses of the drug. The blood levels and urinary excretion of amoxicillin were compared with those of ampicillin.View full abstractDownload PDF (731K) -
TOYOZO TAKADA, YOSHIYUKI KOSUGI, MITSUO AKIBA1977 Volume 25 Issue 2 Pages 259-264
Published: February 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSNovel synthesis of pyrrolo [1, 2-α] indoloquinones, indazoloquinones, and related compounds, which seem to possess the same biological activities as those of mitomycins and rifamycin derivatives, are reported. 2-Acetyl-5-methylhydroquinone tosylhydrazone was oxidized with potassium nitrosodisulfonate affording 2-acetyl-5-methyl-1, 4-benzoquinone tosylhydrazone (9). On treatment with amines (pyrrolidine (a), piperidine (b), morpholine (c), and diethylamine (d)), 9 gave 2-acetyl-3-amino-5-methyl-1, 4-benzoquinone tosylhydrazones (10a-d). 2, 3-Dihydro-6, 9-dimethyl-5, 8-dioxo-1H-pyrrolo [1, 2-α] indole and the analogous products (14a-d) were obtained by heating 10a-d at their melting points without a solvent. Along with 14a-d, ditolyl disulfide, ditolyl thiolsulfonate and 4, 7-dihydroxy-3, 6-dimethyl-1-tosyl-1H-indazole (16) were obtained as minor products in all these cases.View full abstractDownload PDF (780K) -
MOTONOBU ICHINO, KIYOMI KIKUGAWA1977 Volume 25 Issue 2 Pages 265-270
Published: February 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTreatment of O2, 2'-cyclocytidine hydrochloride (I) with lithium azide in dimethylformamide at an elevated temperature gave 6, 2'-triazacyclocytidine (II) (47.5%) and 2'-azido-2'-deoxycytidine (III) (10.8%). The structure of II was confirmed by physicochemical experiments.View full abstractDownload PDF (785K) -
TATSUO HAMADA, OSAMU YONEMITSU1977 Volume 25 Issue 2 Pages 271-275
Published: February 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSOn irradiation of tryptophan and tyrosine in aqueous solutions with the 2537 Å light in the presence of chloroacetamide, photoalkylations of both amino acids proceeded with the same quantum yield of 0.10. Quenching rate constants (kq) of the fluorescences of tryptophan and tyrosine with chloroacetamide were determined to be 4.0-4.5×109 and 4.0×109 M-1sec-1, respectively. Almost no difference between both kq can explain the same reactivity of tryptophan and tyrosine. In an equimolar mixture, the reactivity of tryptophan was about 7 times that of tyrosine, and this reflects the ratio of extinction coefficients of both amino acids at 2537 Å. In a mixture of several amino acids, if the photolysis was stopped when tryptophan disappeared less than 20%, all amino acids except tryptophan were recovered almost quantitatively. Wavelength dependence of this photolysis was finally examined. On irradiation of the 303 nm light, quantum yield for disappearance of tryptophan was also 0.10, whereas that of tyrosine was almost nil.View full abstractDownload PDF (533K) -
ATSUSHI SUGII, KUMIKO HARADA, NAOTAKE OGAWA1977 Volume 25 Issue 2 Pages 276-279
Published: February 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAn evaluation of a porous polymer containing hydrazide groups as a subtractor for aldehydes and ketones in gas chromatography was described. Reactive species were subtracted in the gas phase due to the formation of hydrazone derivatives on the polymer and could be identified by their absence in the chromatograms. The proposed stationary phase had selectivity for aldehydes and ketones, while alcohols, esters, ethers, halides, hydrocarbons and water showed no effect.View full abstractDownload PDF (521K) -
TSUNEHIRO KITAGAWA, TAKAKO MIURA, KOUJIROU MORI, HYOZO TANIYAMA, KEIIC ...1977 Volume 25 Issue 2 Pages 280-284
Published: February 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe 13C-nuclear magnetic resonance spectra of viomycin, dihydroviomycin and broxoviomycin were measured. Most of the resonance lines in their spectra were assigned on the basis of the spectra of constituted amino acids. The spectra were reasonably interpreted by the proposed structures of viomycin and its derivatives.View full abstractDownload PDF (619K) -
HIROSHI IWASE, ASAO MURAI1977 Volume 25 Issue 2 Pages 285-291
Published: February 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe fragmentation of 46 kinds of N-trifluoroacetyl-L-prolyl amino acid n-butyl esters upon electron impact is investigated for the ultramicrodetermination of amino acids by mass fragmentography. It is found that ion at m/e 166 is the common and base peak for most of the amino acid. Characteristic ions for each α-amino acid are observed at m/e (M-101) or (R+29). Using mass fragmentography monitored at m/e 166, about 10-10 g of amino acids can be detected.View full abstractDownload PDF (780K) -
YOSHIFUMI MAKI, TOKIYUKI HIRAMITSU1977 Volume 25 Issue 2 Pages 292-298
Published: February 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThermolysis of pyrimido-1, 4-benzothiazine sulfonium ylides caused competitively [1, 2] and [1, 4] rearrangements, or β-elimination, depending upon the natures of the substituents in the ylide moiety. Ultraviolet irradiation of the methyl, ethyl and benzyl sulfonium ylides resulted exclusively in the [1, 2] rearrangement followed by ring expansion leading to pyrimido-1, 4-benzothiazepines. On the basis of some data, the reaction sequences of these rearrangements were discussed.View full abstractDownload PDF (889K) -
KIICHI ARAKAWA, TADASHI MIYASAKA, KAZUE SATOH1977 Volume 25 Issue 2 Pages 299-306
Published: February 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSEleven 6-methyl- and 6-phenyl-thiazolo [3, 2-b] pyridazin-4-ium perchlorates (I) are synthesized by acid-cyclization of the corresponding ketosulfides (VI) and thioacetonitriles (VII) which are prepared from 6-methyl-and 6-phenyl-pyridazine-3 (2H) thiones (IVa, b) by alkylation with α-haloketones (V) and α-chloroacetonitrile, respectively. Treatment of the quarternary salts (I) with potassium hydroxide or secondary amines furnishes 2-(2-mercaptovinyl) pyridazine-3 (2H)-ones (XII), nucleophilic attack of the hydroxide ion taking place at the C8a-position of the thiazolo [3, 2-b] pyridazinium system.View full abstractDownload PDF (1009K) -
KAZUE SATOH, TADASHI MIYASAKA, KIICHI ARAKAWA1977 Volume 25 Issue 2 Pages 307-313
Published: February 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTreatment of thiazolo [3, 2-b] pyridazinium perchlorates (I) with potassium cyanide in water-acetonitrile furnishes 8-cyano-4, 7-dihydrothiazolo [3, 2-b] pyridazine-7-ones [II] and anhydro-7-cyano-5, 8-dihydro-8-oxothiazolo [3, 2-b] pyridazinium hydroxides (III), the structure of which are elucidated by chemical properities, infrared, nuclear magnetic resonance, ultraviolet and mass spectrometry, and elemental analysis. Examination of the reaction by conducting under nitrogen or oxygen stream and with or without water as the solvent and by monitoring the presence of organic free radical by means of electron spin resonance spectroscopy suggests that the reaction is initiated by the nucleophilic attack of the cyanide either at C8- or C7-position of the pi-deficient thiazolo [3, 2-b] pyridazinium system (I), followed by incorporation of the atmospheric oxygen to form hydroperoxide via radical anion species.View full abstractDownload PDF (805K) -
SYUICHI KASAI, MASUMI KOISHI1977 Volume 25 Issue 2 Pages 314-320
Published: February 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSEthylcellulose microcapsules containing magnesium aluminum hydroxide hydrate were prepared by the phase separation method using organic polymer solutions and observation on the formation mechanism of wall film during the microencapsulation process was done. The system of ethylcellulose-dichloromethane-n-hexane was used for microencapsulation. In this system, it was found that coacervate drops deposited first on the hydrophobic surface of the core material and the wall was then formed. Furthermore, the region of constant wall thickness was observed irrespective of the weight of ethylcellulose in the microcapsules finally obtained.View full abstractDownload PDF (1784K) -
TETSUJI KAMETANI, TATSUSHI OHSAWA, SHOJI HIRATA, MANAKKALSIVARAMAN PRE ...1977 Volume 25 Issue 2 Pages 321-326
Published: February 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPermanganate oxidation of 12-chloro-5, 6, 7, 7a-tetrahydro-2, 3, 9, 10-tetramethoxy-7-methylindeno [2, 1-α] [3] benzazepine (5) in the presence of piperidine gave the diketospirobenzylisoquinoline (11) and the lactone (15), the latter of which was converted into erythro-and threo-phthalideisoquinoline (16 and 17). 2, 3-Dihydro-7, 8-dimethoxy-5-(2, 3-dimethoxybenzoyl)-3-methyl-1H-3-benzazepine (4) was prepared from N-β-(3, 4-dimethoxyphenethyl)-2, 3-dimethoxyphenylacetamide (26) in four steps.View full abstractDownload PDF (784K) -
SHIKIFUMI KITAZAWA, TETSUO KOMURO1977 Volume 25 Issue 2 Pages 327-337
Published: February 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe present work was designed to make clear a mechanism of fasting-induced reduction in the in situ intestinal absorption of sulfanilamide. Physiological characteristics of fasting in rats were investigated with attention to homeostatic fluid transfer within body. An increase in arterial hematocrit was found to be in proportion to the duration of fasting, which indicates unphysiological conditions in internal fluid environment of body. The method was consisted of intensive monitorings of both the ratio in the transmucosal fluid movement and the arterial hematocrit of the subjected animals during the course of the intestinal perfusion experiments. There observed significant depressions in the transmucosal fluid movement and also in the fluid transfer across the capillary wall in 60-hour-fasted rats as compared with non-fasted controls. These results suggest that fasting induced a fall in both the rate and extent of water exchange between fluid compartments in body, and secondary resulted in the depression of intestinal sulfanilamide absorption.View full abstractDownload PDF (1290K) -
SHIGEO UKAI, KAZUO HIROSE, TADASHI KIHO, CHIHIRO HARA1977 Volume 25 Issue 2 Pages 338-344
Published: February 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe acidic heteroglycans (AC and BC) have been isolated from the fruit bodies of Tremella fuciformis BERK, which grow in China. The structures of the AC- and BC polysaccharides containing D-xylose, D-mannose, D-glucuronic acid and O-acetyl groups were investigated by Smith degradation and methylation analysis. These results indicated that AC and BC were composed of α-1→3 linked D-mannopyranose backbone having highly branched points. D-Glucopyranosyluronic acid end groups, D-xylopyranose end groups and β-1→2 or β-1→3 linked D-xylopyranose side chains were linked to the position 2 of the mannopyranose main chain. Also, the results of Smith degradation suggest that O-acetyl groups are probably located at the glucuronic acid residues. The results indicated that the structures of the polysaccharides, AC and BC, are essentially similar. However, significant difference between AC and BC has been observed in that the ratio of the xylose residues as end groups directly linked to the mannose backbone to the xylose side chains in BC is somewhat higher than that in AC, and the proportion of glucopyranose residues as end groups in BC is slightly larger than that in AC.View full abstractDownload PDF (960K) -
YUKIO SUGIURA, TAKANOBU KIKUCHI, HISASHI TANAKA1977 Volume 25 Issue 2 Pages 345-349
Published: February 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new blue colored penicillamine-Mo complex was obtained at pH 9.2 under a reduction with sodium borohydride. This complex gives electron spin resonance signal which has high level of a monomeric Mo, and shows absorption maxima at 440 and 630 nm which could be assigned to d-d transitions arising from a 4A2g ground state. By an aeration, the Mo complex is oxidized to the yellow colored dioxo-bridged MoV complex. The catalytic activity of the penicillamine-Mo complexes has been investigated by the reduction of acetylene to ethylene and ethane in the presence of borohydride.View full abstractDownload PDF (664K) -
SADAO NISHIGAKI, NORIKO MIZUSHIMA, KEITARO SENGA1977 Volume 25 Issue 2 Pages 349-352
Published: February 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTreatment of ethyl 1, 4-dihydro-1-ethyl-7-methyl-4-oxo-1, 8-naphthyridine-3-carboxylate (1) with selenium dioxide afforded a mixture of ethyl 1, 4-dihydro-1-ethyl-7-formyl-4-oxo-1, 8-naphthyridine-3-carboxylate (2) and 1, 4-dihydro-1-ethyl-7-formyl-4-oxo-1, 8-naphthyridine-3-carboxylic acid (3). Condensation of 2 or 3 with respective amines provided the corresponding N-(1, 4-dihydro-3-ethoxycarbonyl-1-ethyl-4-oxo-1, 8-naphthyridin-7-yl) methylenamine (4-15) and N-(3-carboxy-1, 4-dihydro-1-ethyl-4-oxo-1, 8-naphthyridin-7-yl) methylenamine (16-27), respectively. These compounds were tested for in vitro antibacterial activity.View full abstractDownload PDF (525K) -
MAMORU SUGIURA, KAZUYUKI HIRANO, SHIRO IINO, HIROSHI SUZUKI, TOSHITSUG ...1977 Volume 25 Issue 2 Pages 352-354
Published: February 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe degree of the inhibition of alkaline phosphatases from human placenta and intestine by inorganic phosphate was examined and its results showed an additional difference in alkaline phosphatases between human placenta and intestine in the inhibition by inorganic phosphate.View full abstractDownload PDF (488K) -
TOHRU HINO, MASAKATSU TONOZUKA, YOICHI ISHII, MASAKO NAKAGAWA1977 Volume 25 Issue 2 Pages 354-358
Published: February 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSReaction of 3-tert-butylindole (1a) with NBS in acetic acid gave 3-tert-butyloxindole (2a) and 6-bromo-3-tert-butylindole (3a) instead of 2-bromo derivative (5a). Reactions of 1-acetyl-(1b) and 1-tert-butyl-(1c) derivatives under similar conditions gave 3-bromooxindole (6b) and the brominated indole (7) respectively. On the other hand reaction of 1a with NBS in boiling carbon tetrachloride in the presence of benzoyl peroxide gave unstable 5a as a main product. Reaction of 1b under similar condition did not proceed, but 1c gave 7 as a main product.View full abstractDownload PDF (674K) -
MASATAKA ICHIKAWA, TAKUZO HISANO1977 Volume 25 Issue 2 Pages 358-361
Published: February 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS2-(2-Pyridyl) benzimidazole and 5 (or 6)-substituted derivatives were synthesized by the condensation of p-substituted-o-phenylene diamines with α-picoline in the presence of sulfur or with picolinic acid. These acid dissociation constants were measured in aqueous buffers at 20°by spectrophotometry and fitted the Hammett equation with the use of σpara (ρ=1.3). On the other hand, 2-(2-pyridyl) benzimidazole was nitrated to give its mono-nitro compound which was identical with 5 (or 6)-nitro-2-(2-pyridyl) benzimidazole obtained from p-nitro-o-phenylene diamine. The correlation of the position of substituent groups with their effects for the acidity of 2-(2-pyridyl) benzimidazoles was discussed.View full abstractDownload PDF (521K) -
YUICHI KANAOKA, TETSUO TAKAHASHI, HITOSHI NAKAYAMA1977 Volume 25 Issue 2 Pages 362-363
Published: February 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS7-Amino-4-methylcoumarin (2) was proposed as a candidate key fluorogenic amine. Thus 7-L-leucyl-4-methyl-coumarinylamide (hydrochloride) (1) was prepared and shown to be a useful fluorogenic substrate for the assay of aminopeptidase.View full abstractDownload PDF (364K) -
HEIHACHIRO TAGUCHI, YUKINOBU IKEYA1977 Volume 25 Issue 2 Pages 364-366
Published: February 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTwo new schizandrin type lignans, gomisin F (I) and G (II), were isolated from the fruits of Schizandra chinensis BAILL. (Schizandraceae). Their structures including the absolute configurations were established by chemical and spectral evidences. The absolute structures of gomisin A (V), B (VI), and C (VII), whose relative structures have already elucidated, were also established by circular dichroism spectral studies.View full abstractDownload PDF (431K) -
TOSHIO NAMBARA, TOUICHI TANAKA, MITSUTERU NUMAZAWA1977 Volume 25 Issue 2 Pages 367-368
Published: February 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn order to obtain the optically specific antiserum used for radioimmunoassay of l-pentazocine a hapten-carrier conjugate was prepared from l-pentazocine 2'-carboxymethyl ether by coupling with bovine serum albumin employing the mixed anhydride technique. The antiserum elicited in the rabbit by immunization with this antigen was found to be highly specific to l-pentazocine.View full abstractDownload PDF (368K) -
YUKIO SUGIMURA, KIMIO IINO, YUJI IWANO, TOKIO SAITO, TETSUO HIRAOKA1977 Volume 25 Issue 2 Pages 369-370
Published: February 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS7α-Methoxy-7β-vinylacetamidocephalosporins were synthesized from 7β-(ω-halocrotonyl) aminocephalosporins using phosphorus pentachloride and lithium methoxide by a 1, 6-elimination reaction.View full abstractDownload PDF (329K)
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