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Atsushi Momose, Katsutoshi Kamei, Yoshihiro Nitta
1966 Volume 14 Issue 3 Pages
199-206
Published: March 25, 1966
Released on J-STAGE: March 31, 2008
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Treatment of 1-O-acety1-2, 5-di-O-benzoyl-and 5-O-benzoyl-1, 2-di-O-acety1-β-D-glucuronolactones with aluminum chloride or titanium tetrachloride afforded the corresponding anomeric 1-chloro-1-deoxy derivatives, respectively. 1-Bromo-1-deoxy-2-O-acetyl-5-O-benzol derivative was obtained from reaction of 1-O-acetyl-2, 5-di-O-benzoyl-β-D-glucuronolactone with hydrogen bromide. These compounds are very stable.
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Isoo Ito, Taisei Ueda, Ethuyoshi Kurokawa
1966 Volume 14 Issue 3 Pages
207-211
Published: March 25, 1966
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As a part of studies on syntheses of pyrazolone derivatives, syntheses of 1-phenyl-2-methyl-3(or 4)-[(5-substituted-2, 4, 6-trioxohexahydro-5-pyrimidinyl) methyl]-4(or 3)-substituted-3-pyrazolin-5-one were described.
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Kenji Suzuki, Mariko Asaka, Takashi Abiko
1966 Volume 14 Issue 3 Pages
211-216
Published: March 25, 1966
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The three analogs of bradykinin is described in which the L-serine 6-position has been substituted with L-leucine, O-acetyl-L-threonine, and L-threonine. The biological activity of these analogs were compared with that of bradykinin.
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Kenji Suzuki, Takashi Abiko, Mariko Asaka
1966 Volume 14 Issue 3 Pages
217-225
Published: March 25, 1966
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An alternate synthesis of bradykinin and the synthesis of three analogs of bradykinin is described, in which 4 glycine has been substituted with L-leucine and 6 L-serine has been substituted with O-acetyl-L-serine. The biological activity of three analogs were compared with that of bradykinin.
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Hisashi Nogami, Tsuneji Nagai, Tokao Kasai, Toshio Kajima
1966 Volume 14 Issue 3 Pages
225-232
Published: March 25, 1966
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Commercial DAHG J. P. was kept in various concentrations of aqueous ammonia and the following results were obtained. 1. When the sample was aged in aqueous ammonia, a temporary acceleration of the neutralizing rate was observed at an early stage of the aging process, as was similar to the results obtained in the previous paper. 2. The process of aging was composed of two steps : an increase of the diffraction around 36∼42°of 2θ value and an appearance and development of the peak at 18∼20°of 2θ. The former is considered to be related with the temporary acceleration of the neutralizing rate. 3. Depending on the concentration of aqueous ammonia, the aging product was different, and especially in the case of 28% aqueous ammonia, it resembled to nordstrandite. 4. The growth rate of crystal on the aging, in the case of 28% aqueous ammonia, was explained by the existing experimental equation, i. e., by equation(1). 5. The infrared absorption around 3400 cm
-1 was sharp compared with that of the aged sample in various atmosphere under relative humidity in the previous paper, and it was recognized to be shifted remarkably to 3700 cm
-1.
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Masao Tomita, Hiroshi Furukawa, Tohru Kikuchi, Akira Kato, Toshiro Ibu ...
1966 Volume 14 Issue 3 Pages
232-237
Published: March 25, 1966
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The mass spectra of several benzylisoquinoline alkaloids were examined and the fragmentation mechanism was discussed.
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Akira Takamizawa, Kentaro Hirai, Shinzaburo Sumimoto
1966 Volume 14 Issue 3 Pages
238-243
Published: March 25, 1966
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cis-and trans-2-Methoxymethylene-3-ethoxypropiontirile and 2-ethoxymethylene compounds are successfully separated and their structures were determined. Corresponding ester derivatives were not able to separate, however, the ratio of cis/transformation was made clear by elimination of ethyl alcohol from corresponding acetal compounds.
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Kenji Koga, Hisayuki Matsuo, Shun-ichi Yamada
1966 Volume 14 Issue 3 Pages
243-246
Published: March 25, 1966
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Stereoselective synthesis of l-norephedrine hydrochloride (XI) was investigated starting from D-phenylalanine (D-I), by making use of the comparable configuration at the α-carbon in D-I with the asymmetric center bearing the amino group in XI. The synthetic route is shown in Chart 2.
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Ken'ichi Takeda, Kaname Hamamoto, Kusuo Horiki, Etsuko Honda
1966 Volume 14 Issue 3 Pages
247-255
Published: March 25, 1966
Released on J-STAGE: March 31, 2008
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Since metagenin (Ia) and nogiragenin (IIa) have inherently 11α-hydroxyl group, both of them seemed to be the most convenient starting materials for the synthesis of cortical hormone intermediates. Several kinds of intermediates were prepared and during the course of syntheses of them, an easy dehydration of the 11α-hydroxyl grouo was found.
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Keiji Ito, Keiji Sekiguchi
1966 Volume 14 Issue 3 Pages
255-262
Published: March 25, 1966
Released on J-STAGE: March 31, 2008
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Solubilities of the molecular compound of sulfanilamide and sulfathiazole in aqueous solutions containing varying amounts of sulfanilamide were determined. It was found from the results that the solubility product principle can be applied to such mixtures. Based on the principle, a method for calculating the value of the saturated concentration of the compound was proposed. Besides, the influence of each one of the sulfonamides to solubility of the other was investigated. Using all these data, the phase diagram of the system of sulfanilamide, sulfathiazole and water was constructed which indicates that the system belongs to type where a one-to-one molecular compound is formed but is decomposed by water. It was also confirmed that the metastable solubilities of the compound observed in water and in the sulfanilamide solution can be represented by the points on the extention of the saturation curve of the molecular compound in the diagram.
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Tetsuo Hiraoka, Issei Iwai
1966 Volume 14 Issue 3 Pages
262-268
Published: March 25, 1966
Released on J-STAGE: March 31, 2008
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Total synthesis of estrone by the double cyclization of an acetylenic compound was achieved. This method consists of building up B and C rings of the steroidal skeleton in one step starting from a compound having A and D rings of the future steroidal system. Actually treatment of 2-methyl-2-[6-(m-methoxyphenyl)-2-hexynyl]-1, 3-cyclopentanedione (XII) with polyphosphoric acid successfully gave 3-methoxyestra-1, 3, 5 (10), 8, 14-pentaen-17-one (XIII)which is a key intermediate to estrone, whereas this type of the double cyclization of a symmetrically disubstituted acetylenic compound, 1, 6-bis (m-methoxyphenyl)-3-hexyne (XIII), proceeded in a different way giving the undesirable tetracyclic spirane derivative (IV).
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Shigeru Sako, Takanobu Itai
1966 Volume 14 Issue 3 Pages
269-275
Published: March 25, 1966
Released on J-STAGE: March 31, 2008
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Reaction rates of 3-, 4-, 5-, and 6-chloropyridazine 1-oxides and other halogenopyridazine 1-oxides with piperidine and with sodium ethoxide were measured. The rates and derived parameters were compared. The rate order of position reactivity was 5>3>6>4.
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Shigenobu Okuda, Masafumi Yoshimoto, Kyosuke Tsuda
1966 Volume 14 Issue 3 Pages
275-279
Published: March 25, 1966
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Didehydromatrine (III) was reduced to (±)-allomatrinol (VI') and (±)-matrinol (VII'), and the latter of which was converted to N-benzoyl derivative (VIII'). The optical resolution of VI' and VIII' were carried out by means of dibenzoyl-(+)-tartaric acid. N-Benzoyl-(+)-matrinol (VIII) was transformed to (+)-matrinol (VII) via hydrogenolysis. (+)-Matrinol (VII) and (+)-allomatrinol (VI) were derived into (+)-matrine (I) and (+)-allomatrine (V) by oxidation and successive cyclization.
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Manabu Fujimoto, Makiko Sakai
1966 Volume 14 Issue 3 Pages
280-284
Published: March 25, 1966
Released on J-STAGE: March 31, 2008
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La structure des derives bis-sulfonyles d'amino-3 halo-4 methyl-5 isoxazol a eteconfirmee chimiquement comme les imides bis-sulfonylees correspondantes en position 3, sans aucune possibilite comme des composes en genre de sulfonyl-2 sulfonylimino-3 halo-4 methyl-5 isoxazoline-4. Une methode nouvelle de preparation de la Sulfiodizole N
1-acetylee ou benzoylee a ete presentee au depart de nitro-4 N-(methyl-5 isoxazolyl-3)-benzenesulfonamide, au moyen d'iodination, acylation, et reduction de nitro a l'amine primaire, successivement.
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Akira Kasahara, Takeshi Onodera, Haruo Tachizawa, Yasuo Oshima, Masao ...
1966 Volume 14 Issue 3 Pages
285-292
Published: March 25, 1966
Released on J-STAGE: March 31, 2008
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Various biological effects of androfurazanol, 17β-hydroxy-17α-methyl-5α-androstano[2, 3-c]furazan, were tested on rats and rabbits as compared wity those of stanozolol, 17β-hydroxy-17α-methyl-5α-androstano[3, 2-c]pyrazole. Androfurazanol was practically devoid of estrogenic effect and was aproximately less active than testosterone propionate in estrous inhibition and gonadotropin inhibition. The gonadotropin-inhibiting effect of the compound is supposed to play an important role in the appearance of estrous inhibition. Furthermore the compound was found to be 0.036 times as active as progesterone in progestational activity. The inhibitions of growth and adrenal weights due to cortisone acetate were antagonized by androfurazanol. The result was comfirmed also with histological examinations of the adrenals. Subcutaneous injection of androfurazanol showed a tendency to decrease the urine volume, and sodium and potassium excretions in doses of 0.1 and 2mg. but the changes were not statistically significant. Intraperitoneal LD
50 was 0.494 g./kg. and oral LD
50 2.330 g./kg. but all the animals given this compound by subcutaneous injection survived over 2 weeks even in a dose of 4 g./kg.
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Yoshinori Kidani, Kenji Ukai
1966 Volume 14 Issue 3 Pages
293-296
Published: March 25, 1966
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Synthese of 1- and 2-mercaptophenazine derivatives were carried out by reacting chlorophenazine derivatives with thiourea and its potassium salts were confirmed as their mercaptomethyl and 2, 4-dinitrophenyl ether derivatives.
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Isoo Ito, Noriichi Oda
1966 Volume 14 Issue 3 Pages
297-298
Published: March 25, 1966
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For pharmacological evaluation, diethyl 3-oxo-1, 4-dimethyl-2-phenyl-1, 2, 6, 7-tetrahydro-3H-pyrazolo[4, 3-c]pyridine-6, 6-dicarboxylate was synthesized by the Bischler-Napieralski type of reaction, from diethyl 2-acetamido-2-[(2-methyl-5-oxo-1-phenyl-3-pyrazolin-3-yl)methyl] malonate.
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Nobusuke Kawano, Hiroshi Miura, Eiko Matsuishi
1966 Volume 14 Issue 3 Pages
299-300
Published: March 25, 1966
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Genkwanin (I) was prepared from apigenin trimethyl ether (II) by partial demethylation wity hydrogen iodide.
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Hiroshi Mitsuhashi, Kazunori Shibata, Namio Uehara
1966 Volume 14 Issue 3 Pages
301-303
Published: March 25, 1966
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Shigeru Sako
1966 Volume 14 Issue 3 Pages
303-306
Published: March 25, 1966
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N-oxidation of 5-amino-3, 4-dichloropyridazine and 4-amino-3, 5-dichloropyridazine gave their 1-oxides. The amino groups on 3-, 4-, 5-, and 6-positions of pyridazine 1-oxide were substituted with chlorine or bromine by diazotization, but yield of 3-bromopyridazine 1-oxide was poor. 5-Amino-3, 4-dichloropyridazine 1-oxide is usable as the starting material for the preparation of 5-substituted pyridazine 1-oxides.
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Masaichiro Masui, Hiroteru Sayo
1966 Volume 14 Issue 3 Pages
306-308
Published: March 25, 1966
Released on J-STAGE: March 31, 2008
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Election spin resonance measurements were performed at X-band frequencies using a spectrometer Model JES-3B-365, manufactured by the Japan Electron Optics Co., employing 100 kc. field modulation. The cell for electrogeneration was similar to that used by Adams, et al. Generations were performed in the microwave cavity of the ESR spectrometer using the technique of Geske and Maki. Hyperfine coupling constants were measured by careful comparison with the splitting of Mn
2+in magnesium oxide. The value of 86.8 gauss was taken for the Mn
2+splitting. Preparation and purification of polynitroparaffins were previously given. Samples were dissolved in 50% aqueous acetonitrile solution containing 0.1M potassium chloride as the supporing electrolyte to 5mM. Cathode potentials were controlled against a saturated calomel electrode. Oxygen in the cell and dissolved in the solution was removed by purified nitrogen gas. We thand Japan Electron Optics Co. for measurement of ESR spectrum.
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Koichi Shuko, Mitsutaka Natsume, Toshihiko Okamoto
1966 Volume 14 Issue 3 Pages
311-313
Published: March 25, 1966
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Seiichi Saito, Hiroshi Yoshikawa, Yasuhiko Sato, Hideo Nakai, Norio Su ...
1966 Volume 14 Issue 3 Pages
313-314
Published: March 25, 1966
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Shigenobu Okuda, Masafumi Yoshimoto, Kyosuke Tsuda, Nobuyuki Utzugi
1966 Volume 14 Issue 3 Pages
314-318
Published: March 25, 1966
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