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Robert C. Tweit, Edward A. Brown, Stephen Kraychy, Seth Mizuba, R.D. M ...
1964 Volume 12 Issue 8 Pages
859-865
Published: August 25, 1964
Released on J-STAGE: March 31, 2008
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The preparation, by microbiological methods, of some derivatives of 3-(3-oxo-17β-hydroxy-4-androsten-17α-yl)propanoic acid lactone, hydroxylated at 1β, 2β, 6β, 7α, 7β, 9α, 11α, 11β, 12β, 14α, 15α, or 15β, is described as well as of two 19-nor compounds. Some of these compounds block the effects of deoxycorticosterone acetate on the rat kidney.
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Yoshihisa Mizuno, Tokuo Itoh, Kazuko Saito
1964 Volume 12 Issue 8 Pages
866-872
Published: August 25, 1964
Released on J-STAGE: March 31, 2008
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The evidences that the reported 6-chloro-3, 4-diaminopyridine was actually 2-chloro-3, 4-diaminopyridine (X) were presented. By employing X 4-amino-1H-imidazo[4, 5-c]-pyridine (IV) was prepared via 4-chloro-1H-imidazo[4, 5-c]pyridine (III). An alternative synthetic method leading to IV was devised using 1H-imidazo[4, 5-c]pyridine 5-oxide (II) as a key intermediate as follows. Oxidation of 1H-imidazo[4, 5-c]pyridine (I) with hydrogen peroxide in acetic acid afforded the cerresponding 5-oxide (II); treatment of II with boiling phosphoryl chloride gave rise to III. 3-Nitro-2, 4-dichloropyridine, useful intermediate for the synthesis of IV (via 3-nitro-2, 4-diaminopyridine→2, 3, 4-triaminopyridine) was prepared by N-oxide-phosphoryl chloride reaction from 3-nitro-4-chloropyridine 1-oxide. Comparison of the several routes leading to IV has been made from a standpoint of the over-all yield.
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Yukio Ishida, Kazuko Hara
1964 Volume 12 Issue 8 Pages
872-877
Published: August 25, 1964
Released on J-STAGE: March 31, 2008
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Carbobenzoxylated peptides containing tyrosine inhibited competitively the action of oxytocin on the isolated rat uterus. Among these peptides carbobenzoxy-L-tyrosyl-L-tyrosinate was the most active and 30.4 times as potent as p-nitrophenol on the molar basis. This peptide had non-competitive inhibitions to ACh and barium chloride, but had more active and competitive antagonism to oxytocin when assayed by using their doseresponse curves. On the other hand, it had no inhibition to the avian depressure by oxytocin and to the raising blood pressure by vasopressin. Di-carbobenzoxy-L-cystinyl-di-L-tyrosine ethyl ester, having a low activity for inhibition of contraction by oxytocin, inhibited about 50 per cent of avian depressure by oxytocin, and almost inhibited the raising blood pressure by vasopressin in dog and rabbit.
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Masaichiro Masui, Hidenobu Ohmori
1964 Volume 12 Issue 8 Pages
877-888
Published: August 25, 1964
Released on J-STAGE: March 31, 2008
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Polarographic reduction processes of Girard hydrazones of aliphatic and aromatic ketones were studied. From the results of controlled potential electrolysis, the two-electron reduction process proposed by Prelog and Hafliger for Girard-T Hydrazones of aliphatic and alicyclic ketones was found to be not correct, and a mechanism shown in scheme (4) containing a four-electron reduction process was proposed instead. In the case of the Girard hydrazones of aromatic ketones, the electrode reaction processes seem to be more complicated than the aliphatic series : A reduction mechanism shown as scheme (6) containing four and two-electron reduction processes has been proposed. These mechanisms can explain the polarographic behaviours of Girard hydrazones most adequately. In connection with this study, ultraviolet absorption spectra of Girard hydrazones were measured under various conditions. The molecular forms of Girard hydrazones under the experimental conditions have been discussed from the results.
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Hiroyuki Inouye, Toshio Arai, Yukiko Miyoshi
1964 Volume 12 Issue 8 Pages
888-901
Published: August 25, 1964
Released on J-STAGE: March 31, 2008
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Die Struktur (I) des Monotropeins, eines fur die Pyrolazeen eigentumlichen Monoterpenglucosids, wurde auf Ground der verschiedenen Abbaureaktionen und der spektroskopischen Daten aufgeklart. Dabei wurde zugleich auch die Struktur (XI) des Asperulosids bestatigt.
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Hiroyuki Inouye, Kaoru Fuji
1964 Volume 12 Issue 8 Pages
901-905
Published: August 25, 1964
Released on J-STAGE: March 31, 2008
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Auf Grund der Befunde daβ das Decarboxylierungsprodukt des Bisdesoxymonotropein-tetraacetats mit dem Bisdesoxyaucubin-tetraacetat identisch ist, die stereochemische Beziehung zwischen Montropein, Asperulosid und Aucubin festgestellt. Daruber hinaus wurde auch die absolute Struktur des Aucubins vorgeschlagen.
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Ken'ichi Takeda, Taichiro Komeno, Norio Tokutake, Yoshiko Kanematsu
1964 Volume 12 Issue 8 Pages
905-910
Published: August 25, 1964
Released on J-STAGE: March 31, 2008
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Some 16β-acetylthio and 16β-alkylthio estrones were prepared by substitution of 16-bromo-17-ketosteroids with sulfur nucleophiles. Both 16α- and 16β-bromoestrone methyl ether gave the same 16β-substituted product. Transformation of these alkylthio estrones into 19-norsteroid derivatives by lithium-ammonium reduction was studied.
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Tetsuzo Kato, Hiroshi Yamanaka, Takuitsu Niitsuma, Kokichi Wagatsuma, ...
1964 Volume 12 Issue 8 Pages
910-916
Published: August 25, 1964
Released on J-STAGE: March 31, 2008
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Reaction of diketene with three of aminopyridine and their N-oxides was examined. 2-Aminopyridine (I) afforded its acetoacetate (II) and 2-methyl-4H-pyrido[1, 2-a]pyrimidin-4-one (III) as a by-product. N-oxide of I (V) afforded its acetoacetate (VI) and 2-[(6-acetoacetomido-2-pyridyl)methyl]-6-methyl-4H-pyran-4-one (VII). 3-Amino isomers (VIII and XI) underwent their acetoacetates (VII and XVIII) respectively. Although 4-aminopyridine 1-oxide (XIV) did not react with diketene, 4-aminopyridine (XVI) afforded 1-(4-pyridyl-3-acetyl-6-methyl-2, 4-(1H, 3H)-pyridinedione (XVII).
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Yoshio Kitahara, Tadahiro Kato
1964 Volume 12 Issue 8 Pages
916-924
Published: August 25, 1964
Released on J-STAGE: March 31, 2008
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The mass spectra of 8, 8-dicyanoheptafulvene and its derivatives, which are considered to belong to a non-benzenoid aromatic compound, were measured. The high degree of aromaticity of 8, 8-dicyanoheptafulvenes was made clear by mass spectrometry. Low mass regions of dicyanoheptafulvene showed the elimination of hydrogen cyanide from parent ion and rearrangement to phenylpropiolonitrile ion. The mass spectra of methoxy dicyanoheptafulvenes showed fragmentation quite different from that of 8, 8-dicyanoheptafulvenes. The structures and fragmentation processes of dicyanoheptafulvenes were discussed.
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Kazuo Tori, Yoshio Hamashima, Akira Takamizawa
1964 Volume 12 Issue 8 Pages
924-937
Published: August 25, 1964
Released on J-STAGE: March 31, 2008
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Nuclear magnetic resonance spectra of many bornane derivatives have been studied. The signals of the three methyl groups in the bornane derivatives were assigned. Substituent effects due to various substituents upon the signal positions of the methyl groups were evaluated and discussed briefly. The effect on the signal position of a methyl group on the bridge carbon is considerably greater when a substituent is exo-oriented than when it is endo. However, and exo-substituent which involves a group possessing a powerful diamagnetic anisotropy such as a phenyl and a carbonyl group does not always give a downfield shift to a methyl signal. In such a case, considerable caution must be exercised when considering the configuration of a substituent.
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Masako Ohnishi, Yutaka Kawazoe
1964 Volume 12 Issue 8 Pages
938-945
Published: August 25, 1964
Released on J-STAGE: March 31, 2008
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The nuclear magnetic resonance spectra of a number of substituted benzenes were measured in carbon tetrachloride and in trifluoroacetic acid and the substituent effect of each substituent was estimated in both media. The results were discussed in connection of the π-electron densities on the ring carbon atoms.
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Tadakazu Tsuji, Takeo Ueda
1964 Volume 12 Issue 8 Pages
946-950
Published: August 25, 1964
Released on J-STAGE: March 31, 2008
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The polyamines which were obtained by the hydrogenation of N-substituted 2-methyl-2-nitropropylamines, were derived to the corresponding guanidine derivatives with S-methylisothiourea sulfate. Some polyamines were not derived to the guanidine compound, but to the sulfates of starting materials. The material 2-methyl-2-nitropropylamines were prepared by the condensation of 2-nitropropane, formaldehyde and amines.
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Takeo Naito, Katsujiro Ueno, Fumiyoshi Ishikawa
1964 Volume 12 Issue 8 Pages
951-954
Published: August 25, 1964
Released on J-STAGE: March 31, 2008
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In the 2-amino-6-substituted-9-β-D-ribofuranosylpurines series, 6-hydrazino (VI), 6-methylhydrazino (VIII), 6-hydroxylamino (VII), 6-methylamino (X), and 6-dimethylamino (XI) derivatives were synthesized by condensation of 6-alkylthioguanosines with respective amines. VI and VII were reduced with Raney nickel to 2, 6-diamino derivative (IX). Similarly, VIII was also reduced with Raney nickel to X.
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Yoshio Sakurai, Mahmoud M. El-Merzabani
1964 Volume 12 Issue 8 Pages
954-958
Published: August 25, 1964
Released on J-STAGE: March 31, 2008
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Seven methanesulfonic esters analogues of aminoglycols were prepared and their autitumor activity was investigated with two kinds of rat tumors. Of these compounds, 3, 3'-dimesyloxy-N-methyldipropylamine (No. 838), was proved to be the most effective and seems to be a promising candidate for clinical trial.
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Haruhiko Yamamoto, Makoto O'hara, Takao Kwan
1964 Volume 12 Issue 8 Pages
959-967
Published: August 25, 1964
Released on J-STAGE: March 31, 2008
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Reactions of benzene, 1, 3-cyclohexadiene, cyclohexene and cyclohexane have been investigated on reduced transition metals by using a gas chromatographic pulse technique. Main interest was placed on the applicability of this technique to a prompt evaluation of the selectivity; the destination of the intermediates in benzene-cyclohexane reaction, when injected in a stream of hydrogen, has been determined by taking advantage of the technique. The hydrogenation selectivity was found to be of the sequence Ni<Co<Fe, being reversed with the conversion activity of 1, 3-cyclohexadiene or of cyclohexene to give cyclohexane and benzene. Quite synonymously the dehydrogenation selectivity was in parallel with the conversion activity. The temperature dependency of the relative selectivity was analyzed on the basis of the steady state approximation of the hydrogenation-dehydrogenation reaction. The general trend of the hydrogenation-dehydrogenation reaction of 1, 3-cyclohexadiene and of cyclohexene has been successfully explained with the potential energy level diagram of the reaction.
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Hiroyuki Inouye, Toshio Arai
1964 Volume 12 Issue 8 Pages
968-971
Published: August 25, 1964
Released on J-STAGE: March 31, 2008
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Die Konfiguration der Methylgruppe im Bisdesoxydihydromonotropein, einem Hydrierungsprodukt des Monotropeins bzw. Asperulosids wurde durch mehrere Abbaureaktionen untersucht, wobei die Richtigkeit der von uns vorgeschlagenen Struktur (II) fur dessen Acetat bewiesen wurde.
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Tatsuhiko Nakano, Masahisa Hasegawa
1964 Volume 12 Issue 8 Pages
971-974
Published: August 25, 1964
Released on J-STAGE: March 31, 2008
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Yoshikazu Kondo, Tsunematsu Takemoto, Kikuo Yasuda
1964 Volume 12 Issue 8 Pages
976-978
Published: August 25, 1964
Released on J-STAGE: March 31, 2008
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Daisuke Satoh, Mieko Horie
1964 Volume 12 Issue 8 Pages
979-981
Published: August 25, 1964
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Hiroshi Mitsuhashi, Tadasi sato, Taro Nomura, Ikuko Takemori
1964 Volume 12 Issue 8 Pages
981-984
Published: August 25, 1964
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Akira Tahara, Ken-ichi Hirao
1964 Volume 12 Issue 8 Pages
984-987
Published: August 25, 1964
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Hisao Tsukamoto, Hidetoshi Yoshimura, Hiroshi Tsuji, Tadashi Watabe
1964 Volume 12 Issue 8 Pages
987-989
Published: August 25, 1964
Released on J-STAGE: March 31, 2008
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