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Minoru Sekiya, Noboru Yanaihara, Toshio Masui
1963 Volume 11 Issue 5 Pages
551-553
Published: May 25, 1963
Released on J-STAGE: March 31, 2008
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Aminomethylation of salicylic acid was carried out by heating together N, N'-methylenebisacetamide and phosphoryl chloride affording 5-aminomethylsalicylic acid. For the identification of this product, 5- and 3-aminomethylsalicylic acid were synthesized by another route using 5- and 3-formylsalicylic acid as starting materials.
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Masao Okamoto, Masayo Yamada
1963 Volume 11 Issue 5 Pages
554-559
Published: May 25, 1963
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Hydrogenation of isoquinolines, 2-methyl-1, 2, 3, 4-tetrahydro-7-isoquinolinol (V), 7-isoquinolinol (VII), 2-methyl-7-methoxy-1, 2, 3, 4-tetrahydroisoquinoline (IV), was carried out in three different ways. It was clarified that 2-methyl-2, 3, 4, 4α, 5, 6, 8, 8α-octahydro-7(1H)-isoquinolone (IX) and a pair of corresponding 2-methyl-decahydro-7-isoquinolinols (VIa and VIb), thus obtained, possessed cis configuration at ring juncture. In addition, hydrolysis products of 7-methoxy-1, 2, 3, 4, 5, 8-hexahydroisoquinoline (X) were discussed.
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Masuo Akagi, Setsuzo Tejima, Masanobu Haga
1963 Volume 11 Issue 5 Pages
559-565
Published: May 25, 1963
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Rates of displacement of primary tosyloxy groups of acetylated carbohydrate derivatives with iodide ion have been measured. The products of the reaction have been isolated in all instances. The displacement reaction is second order and the differences in rate coefficients are discussed by the geometry of transition state.
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Yoshikazu Matsushima
1963 Volume 11 Issue 5 Pages
566-570
Published: May 25, 1963
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Theoretical considerations on the extension of ion exchange method for measuring complex stability constants were made. They are (1) the extension towards lower pH region, making possible to calculate the stability constants of hydrogenated complexes and (2) corrections for the formation of complexes with coexisting substances such as buffer substances. Applying these for the treatments of experimental data on the systems of calcium, strontium, barium and zinc with citrate, stability constants were calculated as listed in Table I.
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TchanGi Bak, Itiro Yoshioka
1963 Volume 11 Issue 5 Pages
571-575
Published: May 25, 1963
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The respiration of Escherichia coli and some other microorganisms was found to be more or less inhibited by phenazine and its derivatives tested. 1-phenazinol, 2-methoxyphenazine and griseolutein B were most inhibitory. The inhibition varied with the respiratory substrates used and it was strongest when malate was used as compared with glucose and succinate. The inhibition was not competitive with substrate concentration. In order to attain maximal inhibition, it was necessary to preincubate the cells with the inhibitors for a certain period of time. The inhibition mechanisms were briefly discussed.
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Hiroshi Ishii, Takehiko Tozyo, Daisuke Satoh
1963 Volume 11 Issue 5 Pages
576-582
Published: May 25, 1963
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Fissions of 14α, 15α-epoxy ring in a cardenolide with perchloric acid and with hydrogen chloride were found to afford 14β-steroids. With the use of these reactions, some D-ring-transformed compounds of digitoxigenin, e.g. 15α-hydroxydigitoxigenin, and 14-chloro-3β, 15α-dihydroxy- and-3β-hydroxy-14β, 15β-epoxy-cardenolides, were synthesized.
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Makoto Suzuki, Yoshiyuki Egawa, Tomoharu Okuda
1963 Volume 11 Issue 5 Pages
582-588
Published: May 25, 1963
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Hydroxycarbonylation of optically active 2, 4-dimethylcyclohexanone with glutarimide-β-acetaldehyde was carried out using N-methylanilinomagnesium bromide as a condensation agent, isocycloheximide, α-epi-isocycloheximide and other isomers of cycloheximide being obtained.
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Yoshiyuki Egawa, Makoto Suzuki, Tomoharu Okuda
1963 Volume 11 Issue 5 Pages
589-596
Published: May 25, 1963
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By condensing aliphatic and alicyclic ketones with glutarimide-β-acetaldehyde, several cycloheximide analogous compounds listed in Table I were synthesized. The paper also dealt with improved synthesis of glutarimide-β-acetaldehyde.
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Mitsuru Furukawa, Takeo Uede
1963 Volume 11 Issue 5 Pages
596-600
Published: May 25, 1963
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4-Amino-6-substituted amino-s-triazine-2-carboxamide was synthesized by reacting 1-substituted 3-(4, 5-dioxo-2-imidazolidinylidene) guanidine, which was prepared in a good yield through the reaction between equimolar amounts of 1-substituted biguanide and diethyl oxalate, with various amines.
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Kiyoshi Takahashi, Masako Muraoka, Takeo Ueda
1963 Volume 11 Issue 5 Pages
601-604
Published: May 25, 1963
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The eight compounds of N-alkyl-4-morpholinecarboxamidine sulfate were synthesized via N-alkyl-4-morpholinethiocarboxamide from alkyl isothiocyanate, wherein alkyl group stands for H, CH
3, C
2H
5, C
3H
7, C
4H
9, C
5H
11, C
6H
13, or cyclohexyl. Any of the compounds synthesized was found inactive on any of polio, measles and influenza virus.
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Keiichi Takamura, Chifuyu Isono, Sakae Takaku, Yoshihiro Nitta
1963 Volume 11 Issue 5 Pages
604-612
Published: May 25, 1963
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17β-(2-alkylamino-(or 2-arylamino- or 2-N, N-alkylarylamino-)-4-thiazolyl) androst-4-en-3-one derivatives were prepared from Reichstein's compound S 21-iodide, cortisone 21-iodide and desoxycorticosterone 21-iodide or corresponding 21-mesylate with N-alkylthiourea, N-arylthiourea or N, N-alkylarylthiourea respectively. Some of these compounds were found to have a digitalis-like properties (cardiac glucoside properties) as a result of pharmacological test.
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Keiichi Takamura, Chifuyu Isono, Shinichi Takama, Yoshihiro Nitta
1963 Volume 11 Issue 5 Pages
613-618
Published: May 25, 1963
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17β-(2-alkylamino-(or 2-arylamino-or 2-N, N-alkylarylamino-) thiazolyl) androst-4-en-3β, 17α-diol was prepared from corresponding 3-one with sodium boronhydride in dioxan or dioxane-methanol (1 : 1). 17β-(2-alkylamino-(or 2-arylamino-)-4-thiazolyl) androst-4-en-3β, 17α-diol 3-(hydrogen succinate) and O, N-bis(hydrogen succinate) were obtained from corresponding 3β, 17α-diol and 17α-ol-3-one with succinic anhydride. Some of this substance had a digitalis like properties.
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Takashi Mitsui, Hiroshi Ozaki, Hiroaki Kumano, Hajime Sano
1963 Volume 11 Issue 5 Pages
619-623
Published: May 25, 1963
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A colorimetric method for the determination of dimethyl 2, 2-dichlorovinyl phosphate (DDVP) is described, which is based on the color complex formed between DDVP and acetone in the presence of ethanolic KOH. The absorption at 370mμ by the color reaction products follows Lambert-Beer's law. This method can be applied to Dibrom and Dipterex, the analogues of DDVP.
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Takashi Mitsui, Hiroshi Ozaki, Etsuko Toda, Hajime Sano
1963 Volume 11 Issue 5 Pages
624-628
Published: May 25, 1963
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A colorimetric method for the determination of DDVP is modified to adapt for the determination of Dibrom, which based on the color complex formed between Dibrom and acetone in the presence of alkali. The values obtained from this method showed good agreement with the values from the infrared absorption spectral method. Periodical change of 5% Dibrom emulsifiable concentrate was studied at 100, 70, 60, and 50° by this colorimetric method, and statistical treatment was made to presume the days required until 10% reduction at 30, 25, and 20°. Experiments were further made to see whether these values would agree when the concentrates were maintained at room temperature. From this result, the days required until 10% reduction at room temperature were 1.5, and 3∼4 months in the emulsifiable concentrate containing 5% of epi-chlorohydrin and the one not containing it, respectively. These values showed good agreement with the values obtained from the statistical treatment. epi-Chlorohydrin has no stabilizing effect on Dibrom or rather promotes decomposition. Dibrom in the emulsifiable concentrate is fairly stable when nonionic emulsifier alone is present, but undergoes fairly rapid decomposition in the presence of anionic emulsifier alone.
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Shigeru Yoshida
1963 Volume 11 Issue 5 Pages
628-638
Published: May 25, 1963
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Infrared absorption spectra of benzamide, p-substituted benzamide, pyridinecarboxylic acid amides, pyrazinamide and their homologs were measured in Nujol mull and in solution, and the assignment of the characteristic absorption has been made. The infrared absorption spectral data suggested the crystal structure of isonicotinamide, α-and β-type of pyrazinamide and β-type of pyrazinamide. 1) Benzamide, p-substituted benzamides, picolinamide (β-type), and pyrazinamide (β-type) showed a similar absorption tendency and are therefore supposed to have a similar crystal structure. β-Type of picolinamide and pyrazinamide is different in symmetric center. 2) Nicotinamide and isonicotinamide showed the same absorption tendency and, therefore, the same crystal structure was formed. 3) Pyrazinamide (α-type) and picolinamide (α-type) showed the same absorption tendency and is supposed to form the same crystal structure.
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Issei Iwai, Tetsuo Hiraoka
1963 Volume 11 Issue 5 Pages
638-643
Published: May 25, 1963
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Intramolecular condensational cyclization of the acetylenic compounds to the aromatic nucleus was achieved with polyphosphoric acid, and this reaction was accompanied with dehydrogenation to give naphthalene derivatives. This method can also be used to nitrogen containing acetylenic compounds to prepare carbostryril derivatives.
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Toshihiko Okamoto, Yutaka Kawazoe
1963 Volume 11 Issue 5 Pages
643-650
Published: May 25, 1963
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The scope and limitations of the spatial interaction effect of the hydroxyl group to the proton magnetic resonance are discussed in details.
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Kiyoshi Sakai, Kyosuke Tsuda
1963 Volume 11 Issue 5 Pages
650-653
Published: May 25, 1963
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Es wird eine partielle Synthese des Brassicasterins beschrieben. Das aus (-)-2R-1-Jod-2, 3-dimethylbutan gewonnene Triphenyl-2, 3-dimethylbutylidenphosphoran laβt sich mit 3-Methoxy-23, 24-dinor-5-cholen-22-al umsetzten. Das hierbei erhaltene 24β-Methylcholesta-5, 22-dien-3β-ol erweist sich nach einem Vergleich mit den Daten in der Literatur als identisch mit Brassicasterin.
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Keijiro Takagi, Yutaka Kasuya, Kyo Fujie, Minoru Watanabe, Setsuko Kay ...
1963 Volume 11 Issue 5 Pages
654-657
Published: May 25, 1963
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Several acids- and aminoacids-derivatives of α-methyl-3, 4-methylenedioxyphenethylamine were synthesized and their analgesic activities in mice were estimated by two methods. The most potent compound was propionamide of the amine (SA-8) and this was 1.4 times more potent than aminopyrine. SA-8 was sedative in mice, and it markedly augmented the hypnotic action of hexobarbital.
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Keijiro Takagi, Yutaka Kasuya, Minoru Watanabe
1963 Volume 11 Issue 5 Pages
658-669
Published: May 25, 1963
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General pharmacology of N-(α-methyl-3, 4-methylenedioxyphenethyl) propionamide (SA-8), previously synthesized by us, was described with emphasis at the effects on central nervous system. SA-8 reduced the spontaneous and methamphetamine-induced locomotor activity of mice rather stronger than meprobamate did. SA-8 did not protect mice from tonic convulsion and death by infused pentylenetet razol. It had hypothermic effect in rast but no antipyretic effect in rabbits at higher doses. SA-8 itself had weak specificity for the conditioned avoidance response in rats, but it markedly potentiated the effect of chlorpromazine on the response. The influence of SA-8 on the EEG in curarized cats was investigated. SA-8, administered intravenously, at small doses (20∼40mg./kg.) depressed spontaneous activities of cortex and hippocampus, but at larger doses (60∼90mg./kg.), it activates cortex and reticular formation, and if further doses were injected, seizure discharges throughout the whole brain occurred. Studies by means of electrical stimulation revealed that SA-8 in small doses depressed the hypothalamic activating system, but that it little affected the reticular activating system in cats. SA-8 antagonized to the depressive effect of hexobarbital on the electrical activity of brain in cats, contrary to the results reported in previous paper that SA-8 prolonged the hexobarbital induced sleep in mice. SA-8 had little spasmolytic activity in vitro in mice. It lowered blood pressure in cats. LD
50 value of orally administered SA-8 was 450mg./kg. (357∼567, p=0.05).
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Fumio Yoneda, Yoshihiro Nitta
1963 Volume 11 Issue 5 Pages
669-673
Published: May 25, 1963
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Bei der Einwirkung von Benzylchlorid auf Maleinsaurehydrazid wurden mono- und dibenzylierte Verbindungen hergestellt. In diesem Zusammenhang wurden verschiedene Benzylderivate des Maleinsaurehydrazides hergestellt. Die Konstitution der oben erhaltenen Benzylderivate wurde vermittels UV-Spektren untergesucht.
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Shunichi Yamada, Tohru Hino, Kiyomi Ogawa
1963 Volume 11 Issue 5 Pages
674-678
Published: May 25, 1963
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Lithium aluminum hydride also was found to be effective as the Ladenburg method for the reductive cyclization of 3-(2-aminoethyl)-, 3-(3-aminopropyl)-1, 3-dimethyl oxindole (IVa and IVc) and their N-methyl derivatives (IVb, IVd) to pyrrolo (and pyrido) [2, 3-b] indole derivatives (Va-Vd). With a little excess of lithium aluminum hydride IVd gave a indoline derivative (VIII) together with the cyclized base (Vd) though the latter of which could not be cleaved by lithium aluminum hydride even under more strenuous condition.
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Yoshikazu Kondo, Tsuneo Ikenoue, Tsunematsu Takemoto
1963 Volume 11 Issue 5 Pages
678-680
Published: May 25, 1963
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Kazuo Tori, Masaru Ogata, Hideo Kano
1963 Volume 11 Issue 5 Pages
681-684
Published: May 25, 1963
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Hiromu Mori, Shunyo Wada, Kiyoshi Tsuneda
1963 Volume 11 Issue 5 Pages
684-685
Published: May 25, 1963
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Yasuhiro Morisawa, Yukichi Kishida, Katsumi Tanabe
1963 Volume 11 Issue 5 Pages
686-687
Published: May 25, 1963
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