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Zen-ichi Horii, Takeshi Inoi, San-Wong Kim, Yasumitsu Tamura, Aritomo ...
1965 Volume 13 Issue 10 Pages
1151-1159
Published: October 25, 1965
Released on J-STAGE: March 31, 2008
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A number of 2-aralkyltetrahydro-1, 3-oxazines, 3-aralkylamino-1-propanols and 3-aralkyltetrahydro-1, 3-oxazines were prepared and their pharmacological activities tested. Some compounds belonging to the last two groups showed higher bronchodilator activities than aminophilline and even than ephedrine. The structures of tetrahydro-1, 3-oxazines prepared were also discussed.
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Hiroshi Morimoto, Isuke Imada
1965 Volume 13 Issue 10 Pages
1160-1163
Published: October 25, 1965
Released on J-STAGE: March 31, 2008
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Die Ubichromenol-Gruppe wurde mit Hilfe der impragnierten Chromatographie qualitativ nachgewiesen. Eine quantitative Bestimmungsmethode an Ubichromenol (35)(IIb) wurde ebenfalls nach einer kombinierten Methode mit Dunnschichromatographie und Extinktionswert bei 332 mμ festgestellt.
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Hiroshi Morimoto, Isuke Imada, Hotsue Nishida
1965 Volume 13 Issue 10 Pages
1164-1167
Published: October 25, 1965
Released on J-STAGE: March 31, 2008
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Ubichromenol (35)(I) wurde in Ratten sc. Injiziert und in der Leter, im Plasma, in den Blutkorperchen sowie in Gehirn quantitativ analysiert. In Lebern, Plasma, und Blutkorperchen lieβ sich I, jedoch im Gehirn nicht nachweisen.
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Tadashi Sasaki, Katsumaro Minamoto
1965 Volume 13 Issue 10 Pages
1168-1177
Published: October 25, 1965
Released on J-STAGE: March 31, 2008
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Im Rahmen der Untersuchungen der Synthesemoglickeit von as-Triazin-N-oxyden, oxydierten wir 3-Amino-5, 6-diphenyl-as-triazin, 5, 6-Diphenyl-as-triazin-3 (2H)-on und ihre einfache Derivate durch Persaure, wobei sich einige entsprechenden 1-N-Oxyde erhalten lieβen, deren Konstitutionen spektroskopisch sowie dipolmomentmetrisch diskutiert wurden.
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Akio Fujita, Jun-ichi Matumoto, Shinsaku Minami, Hideji Takamatsu
1965 Volume 13 Issue 10 Pages
1177-1182
Published: October 25, 1965
Released on J-STAGE: March 31, 2008
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An unusual product, resulted from the reaction of 5-nitro-2-furaldehyde with pyridine or its equivalents in acetic anhydride, was established to be 1, 2-diacetoxy-1, 2-bis (5-nitro-2-furyl) ethene.Similarly, 1, 2-diacetoxy-1, 2-bis (5-nitro-2-thienyl) ethene was obtained from the self-condensation reaction of 5-nitro-2-thenaldehyde. Attempts to prepare the corresponding condensation products of some other aromatic aldehydes, however, failed under the similar reaction conditions.
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Akio Fujita, Tadatsugu Yamamoto, Shinsaku Minami, Hideji Takamatsu
1965 Volume 13 Issue 10 Pages
1183-1193
Published: October 25, 1965
Released on J-STAGE: March 31, 2008
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To test the antibacterial activity, 2- or 4-[2-(5-nitro-2-furyl) vinyl] pyrimidines were synthesized by the condensation of 5-nitro-2-furaldehyde (Va) with the active methyl group of pyrimidines. It has been found that Va predominantly condensed with the 4-methyl group of 2, 4-dimethylpyrimidine and in the reaction of Va with 2, 4-dimethylpyrimidine containing a functional group in the 6-position, the active hydrogen reactivity between the 2-methyl group and 4-methyl group is affected by the presence of group in the 6-position : in 2, 4-dimethylpyrimidines substituted by the hydroxy, amino and alkoxy group in the 6-position, the 2-methyl group was founded to be more active, while in the ones substituted by the acetamido, dimethylamino and chloro group, the 4-methyl group was more reactive.
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Osamu Tamemasa, Shoji Okada, Yasuo Wakita
1965 Volume 13 Issue 10 Pages
1193-1199
Published: October 25, 1965
Released on J-STAGE: March 31, 2008
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4-NO
2-Phe and 4-F-Phe exert the inhibiting action to the Phe or Tyr incorporation into proteins of the intact Ehrlich mouse ascites tumor cells. The inhibiting effect of 4-F-Phe is similar in the intact and disrupted tumor cells and the intact liver cells, while the effect of 4-NO
2-Phe is different among these three materials ; little inhibition inthe disrupted tumor cells, and rather stimulation in the whole liver cells. Optimum incubation medium and conditions of these experiments were studied. Finally, the site of bilolgical systems, which is affected by amino acid analogs, is discussed.
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Masuo Akagi, Yoneshiro Oketani, Takayoshi Uematsu
1965 Volume 13 Issue 10 Pages
1200-1206
Published: October 25, 1965
Released on J-STAGE: March 31, 2008
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1) Method was described for the estimation of p-ethoxyphenylurea in biological fluids and tissues. 2) The physiological disposition of p-ethoxyphenylurea was demonstrated in rabbits and rats. p-Ethoxyphenylurea was rapidly absorbed from the gastrointestinal tract, remained long, and was almost competely metabolized in the body.
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Akira Takamizawa, Yoshio Hamashima
1965 Volume 13 Issue 10 Pages
1207-1220
Published: October 25, 1965
Released on J-STAGE: March 31, 2008
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In connection with the study of the acetylation of 7-aminopyrazolo [1, 5-a] pyrimidines, further studies on the acetylation were investigated. Mono- and diacetates were obtained from the compounds being substituted with methyl-, Phenyl-, or ethoxy-carbonyl group at the C-6 position and only monoacetates being unsubstituted or with a cyano group at the C-6 position. The reason for this was confirmed to be the steric effect of the substituents at the C-6 position. Various 7-acylamino (XXXVII∼XL, XLII∼XLVI), 7-alkylamino (XLI, LVIII∼LXVI), and 7-H pyrazolo [1, 5-a] pyrimidines (LIII∼LV) were also derived.
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Tetsuji Kametani, Kazuo Kigasawa, Mineharu Hiiragi
1965 Volume 13 Issue 10 Pages
1220-1224
Published: October 25, 1965
Released on J-STAGE: March 31, 2008
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In order to test the analgesic action of 1-methl-(XIa) and 1, 3-dimethyl-1, 2, 3, 4, 5, 6-hexahydro-2, 6-methanobenzo [d][1, 3] diazocine (XIb) were synthesized from 1-methyl-4-carboxymethylcarbostyril (III) as a starting material. Reductive cyclization of Xa and Xb with metallic sodium in ethanol gave, respectively, the expected azabenzomorphane derivatives, XIa and XIb. Furthermore, Ladenburg reduction of 1-methyl-4-carba-moylmethylcarbostyri (XII) also gave the above compound (XIa).
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Tetsuji Kametani, Kazuo Kigasawa, Tetsutaro Hayasaka
1965 Volume 13 Issue 10 Pages
1225-1230
Published: October 25, 1965
Released on J-STAGE: March 31, 2008
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In order to test the analgesic action of azabenzomorphane derivatives, 4-benzyl-3, 4, 5, 6-tetrahydro-1 H-2, 6-methanobenzo [e][1, 3] diazocine (XVIa) and its 2-phenyl derivative (XVIb) were synthesized by cyclization of 4-(benzylaminomethyl)-1, 2, 3, 4-tetrahydroisoquinoline with paraformaldehyde and benzaldehyde. Both compounds were found to be extremely lavile ahainst acid. Methods for synthesis of VI, which was used as a key intermediate, were also examined using 4-cyanoisoquinoline (II) as a srarting material according to three procedures, namely, a) catalytic hydrogenation of 4-benzylaminoisoquinoline (IV), b) reduction of 4-(benzamidonethyl) isoquinoline (X), and c) hydrogenation of the cyclization product between 4-aminomethyl 1-1, 2, 3, 4-tetrahydroisoquinoline (XV) and benzaldehyde.
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Naoto Yoneda
1965 Volume 13 Issue 10 Pages
1231-1240
Published: October 25, 1965
Released on J-STAGE: March 31, 2008
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12-Methyl-1, 2, 3, 4, 6, 7, 12, 12b-octahydro-2, 6-methanoindolo [2, 3-a] quinolizine (I), which represents the fundamental skeleton of sarpagine type indole alkaloids, was synthesized. Thus methyl ester (XI) hydrochloride of N-benzyl-1-methyltryptophan was treated with methy 3-formylpropionate to form tetrahydro-β-carboline derivative (XV), from which 6, 10-imino-5H-cyclooct [b] indole dervative (XVII) was prepared by Dieckmann cyclization with sodium hydride under a certain working condition. This was condensed with methyl bromoacetate followed by ketone fission to yield ketoester (XX), from which N-benzyl group was reductively removed and then converted to N-methyl derivative (XXIII).The ethylene thioketal (XXV) of the latter was desulfurized as usual and the product was reduced by lithium aluminum hydride to furnish the corresponding alcohol (XXVII), which was tosylated with tosyl chloride in pyridine in the cold. Spontaneous quaternization of the tosylate took place forming the cyclized quaternary base (XXVIII), the chloride salt of which was submitted to pyrolysis reaction to produced the desired base (I).
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Junzo Shoji, Shoji Shibata, Ushio Sankawa, Heihachiro Taguchi, Yoshiko ...
1965 Volume 13 Issue 10 Pages
1240-1246
Published: October 25, 1965
Released on J-STAGE: March 31, 2008
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The structure of erythroskyrine, C
26H
33O
6N, m.p. 130∼133°, [α]
D+46.9°, an orange red pigment of Penicillium islandicum SOPP has been elucidated to be represented by the formula (I).
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Yoshio Arata, Tsutomu Ohashi
1965 Volume 13 Issue 10 Pages
1247-1251
Published: October 25, 1965
Released on J-STAGE: March 31, 2008
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A new alkaloid (I), C
15H
23O
2N has been isolated from Nuphar japonicum DC. and named nuphamine. The compound (III) obtained by the catalytic reduction after the chlorination of I with thionyl chloride is completely in accordance with (-)-desoxynupharamine, derived from nupharamine (IX). By the catalytic reduction of I with palladium-carbon, dihydronuphamine (V), (-)-deoxynupharidine (VI-A) and allodeoxynupharidine (VI-B) were prepared. VI-A and VI-B were also prepared from V. Judging from these reactions and the nuclear magnetic resonance spectra, the structure of I has been determined to be presented by the fromula VIII. The steric chemical correlations among the alkaloids, (-)-desoxynupharidine (VI-A), (-)-nuphamine (VIII) and (-)-nupharamine (IX) isolated from Nuphar iaponicum have been also achieved.
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Sadatake Kato, Kunio Kurata
1965 Volume 13 Issue 10 Pages
1252-1254
Published: October 25, 1965
Released on J-STAGE: March 31, 2008
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A new method to increase radioactive yield in substitutional reaction is deviced and applied to preparation of sodium radio 3, 5-diiodofluorescein (3, 5-
131I). In this method, produced radioisotope of inert form is converted into active form by isotopic exchange reaction and reused for the reaction. The radioactive yield was increased from 43% to 70%.
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Shoji Shibata, Tsutomu Furuya, Hidefumi Iizuka
1965 Volume 13 Issue 10 Pages
1254-1257
Published: October 25, 1965
Released on J-STAGE: March 31, 2008
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The gas-liquid chromatography of zeorin was carried out using free zeorin and its trimethylsilyl ether. The chromatograms were analyzed to discuss the transformation of the compounds during the process.
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Sachiko Kanao, Terumi Nakajima, Zenzo Tamura
1965 Volume 13 Issue 10 Pages
1262-1263
Published: October 25, 1965
Released on J-STAGE: March 31, 2008
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Akira Tanaka, Akira Hasegawa, Goro Urakubo
1965 Volume 13 Issue 10 Pages
1263-1265
Published: October 25, 1965
Released on J-STAGE: March 31, 2008
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Shun-ichi Yamada, Kiyoyasu Ishikawa, Kazuo Achiwa
1965 Volume 13 Issue 10 Pages
1266-1269
Published: October 25, 1965
Released on J-STAGE: March 31, 2008
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Toshihiko Okamoto, Mitsutaka Natsume, Yoichi Iitaka, Akie Yoshino, Tak ...
1965 Volume 13 Issue 10 Pages
1270-1272
Published: October 25, 1965
Released on J-STAGE: March 31, 2008
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