巻号一覧
83 巻, 8 号
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ジケテンとイソニコチン酸ヒドラジドとの反応加藤 鉄三, 山中 宏, 浜口 文子1963 年 83 巻 8 号 p. 741-744
発行日: 1963/08/25
公開日: 2010/02/19
ジャーナル フリーIsonicotinic acid hydrazide (INAH) affords its acetoacetate (IV), when reacted with diketene. IV gives isonicotinopiperidide and 3-methyl-2-pyrazolin-5-one (VII) in the presence of piperidine in ethanol solution, and it also produces VII and isonicotinc acid in the presence of pyridine in acetic acid solution. IV affords INAH and 1-phenyl-3-methyl-2-pyrazolin-5-one (II), when reacted with phersylhydrazine and it also produces VII and 1, 1-diisonicotinoylhydrazine (VIII) in the reaction with INAH. However the cyclization reaction of isonicotinoylpyrazolone (V or VI) was unsuccessful. IV is hydrolyzed into VIII, VII and acetone, emitting carbon dioxide gas. On the other hand, the hydrolysis of IV, after the benzylation, gave 3-methyl-4-benzyl-2-pyrazolin-5-one and isonicotinic acid. The reaction mechanisms is discussed in this report.抄録全体を表示PDF形式でダウンロード (628K) -
7-Aminopyrazolo [1,5-a] pyrimidineおよびそのMethyl置換体の合成高見沢 映, 浜島 好男, 林 貞男, 城戸 良之助1963 年 83 巻 8 号 p. 745-752
発行日: 1963/08/25
公開日: 2010/02/19
ジャーナル フリーBased upon the fact that 7-amino-3, 6-dimethylpyrazoio[1, 5-a]pyrimidirie (XIII) possesses effective antipyretic and analgetic action, 14 methyl substitutes of 7-aminopyrazolo[1, 5-a]-pyrimidine in its nuclei were synthesized.
With 5-aminopyrazoles (VII-X), 2-methyl-3-ethoxy-3-methoxypropionitrile (I) was reacted to give 6-methyl compounds (XI-XIV), acetoacetonitrile (III) was reacted to give 5-methyl derivatives (XV-XVIII), 2-acetopropionitrile (IV) to 5, 6-dimethyl derivatives (XIX-XXII), and ethyl ethoxymethylenecyanoacetate (V) to 6-ethoxycarbonyl derivatives (XXVII-XXX). In this connection, the cyclization with V in both acidic and alkaline media, and the saponification of XXVII-XXX were investigated. The thermal decomposition of XXXV-XXXVIII produced decarboxyl compounds (XXXIX-XLII) easily. Another synthetic method of XLII was also studied.抄録全体を表示PDF形式でダウンロード (1113K) -
梅本 進, 於勢 真輔, 高松 秀二1963 年 83 巻 8 号 p. 753-756
発行日: 1963/08/25
公開日: 2010/02/19
ジャーナル フリーIn order to reduce the side effect of N-phenylacetylureas, hitherto used as anticonvulsants, 1-acyl-3-phenylacetylureas were prepared by acylation of N-phenylacetylureas or by the reaction of acylisocyanates and acylamides. Of the compounds synthesized, 1-acetyl-3-(1-ethylphenylacetyl)urea was found to be a convulsant with small side effect.抄録全体を表示PDF形式でダウンロード (672K) -
オニドコロ根茎の新ステロイドサポニン, YononinおよびTokoronin川崎 敏男, 山内 辰郎1963 年 83 巻 8 号 p. 757-760
発行日: 1963/08/25
公開日: 2010/02/19
ジャーナル フリーIt is known that, among the sapogenins contained in Dioscorea Tokoro MAKINO, majority of yonogenin and tokorogenin are present in a free state in the aerial part. Two kinds of new steroidal saponins with yonogenin and tokorogenin as their aglycones were isolated from the water-insoluble saponin fraction of the rhizome of this plant. These saponins are yonogenin α-L-arabinoside (I), m. p. 238-240° (decomp.), [α]D15-14.5°, and tokorogenin α-L-arabinoside (II), m. p. 270-274° (decomp.), [α]D15-10.6°, which were respectively named yononin and tokoronin.抄録全体を表示PDF形式でダウンロード (643K) -
TrilobineおよびIsotrilobineの構造 その16 Trilobineの構造富田 真雄, 古川 宏1963 年 83 巻 8 号 p. 760-763
発行日: 1963/08/25
公開日: 2010/02/19
ジャーナル フリーThe structure of trilobine was reported by Inubushi and Nomura as the formula (I) from the cleavage reaction of its N-acetyl compound with metallic sodium in liquid ammonia. The antipodal isotrilobine (II) was synthesized from dlhydroepistephanine (V) by the present writers.
In the present series of work, O-methylanhydrodemethyl-N-ethyl-dihydroepistephanine (X) was synthesized from N-ethyldihydroepistephanine (VII) by a similar method. X came as a picrate of m.p. 194-195°, [α]D-283.1° (acetone), C37H38O5N2⋅2C6H3O7N3⋅1 1/2H2O. By comparison with the picrate, m.p. 193-195°, [α]D+283.8° (acetone), C37H38O5N2⋅2C6H3O7N3⋅1 1/2H2O, of the N-ethyl compound (III) from natural trilobine (I), X was found to be its antipode (cf. Table I). Consequently, the structure of trilobine was reaffirmed as I by synthesis.抄録全体を表示PDF形式でダウンロード (574K) -
富田 真雄, 小塚 睦夫, 中川 悦子, 光法 由紀子1963 年 83 巻 8 号 p. 763-766
発行日: 1963/08/25
公開日: 2010/02/19
ジャーナル フリーFrom the barks and woods of Laurus nobilis LINN., Japanese name “Gekkeiju” cultivated in Japan, actinodaphnine (III) and a new secondary aporphine-type base, launobine, C18H17O4N, m. p. 214-215° (decomp.), [α]D21+192.7°, were isolated and the structure of the latter has been certified to be VII.抄録全体を表示PDF形式でダウンロード (695K) -
Thiocyanatopyridazine誘導体の合成および抗菌作用衣川 二郎, 落合 道彦, 山本 弘一1963 年 83 巻 8 号 p. 767-771
発行日: 1963/08/25
公開日: 2010/02/19
ジャーナル フリーA new kind of thiocyanatopyridazine derivatives were synthesized and their antifungal activities were tested. 3-Halogeno-6-thiocyanatopyridazine, 4-thiocyanato-3, 6-dichloropyridazine were found to show the remarkable activity.抄録全体を表示PDF形式でダウンロード (726K) -
諸種2-(5-Nitro-2-furyl) vinyl Heterocyclic体の合成ならびに抗菌性について三浦 孝次, 大橋 冨次, 松田 澄江, 五十嵐 良子1963 年 83 巻 8 号 p. 771-777
発行日: 1963/08/25
公開日: 2010/02/19
ジャーナル フリーA total of 28 kinds of Panfuran-type compounds, in which the nitrofuran and heterocyclic rings are connected through one double bond, were prepared and their antibacterial action was tested with Streptococcus haemolyticus, Staphylococcus aureus, Escherichia coli, Shigella flexineri, and Bacillus subtilis. The quinoline compounds were found to be most effect as a chemotherapeutic and acetamidoquinoline derivative showed the most marked effect, inhibiting bacterial growth of Bacillus subtilis in a very dilute solution of ca. 2, 000, 000, 000 dilution.抄録全体を表示PDF形式でダウンロード (557K) -
特に2-Amino-5-〔2-(5-nitro-2-furyl) vinyl〕-1,3,4-thiadiazoleとSulfamethylthiadiazoleとの溶連菌感染ハツカネズミに対する治療作用比較三浦 孝次, 池田 政男, 五十嵐 良子, 大森 富士雄1963 年 83 巻 8 号 p. 778-780
発行日: 1963/08/25
公開日: 2010/02/19
ジャーナル フリー2-Amino-5-[2-(5-nitro-2-furyl) vinyl]-1, 3, 4-thiadiazole (I) was prepared by the oxidation of nitrofurylacrolein thiosemicarbazone. Eight kinds of similar-type compounds were prepared, and their antibacterial action and therapeutic effect against mice infected with Streptococcus haemolyticus were examined. I had a great effect and its effect was compared with that of sulfamethylthiadiazole (Urocydal), which is known as the urethral infection therapeutic. It was thereby learned that the nitrofuran ring had chemotherapeutic effect even in vivo.抄録全体を表示PDF形式でダウンロード (372K) -
イソニアジド誘導体の分配平衡について中垣 正幸, 奈良 賢一1963 年 83 巻 8 号 p. 781-784
発行日: 1963/08/25
公開日: 2010/02/19
ジャーナル フリーDistribution coefficients of isonicotinoylhydrazone (isoniazone) of calcium pyruvate, sodium pyruvate, glucose, and sodium glucuronate between isoamyl acetate and water at 30° were determined by considering the hydrolysis equilibria of the isoniazones in both phases. For this purpose, the concentrations of INAH, isoniazones, and carbonyl compounds were measured in the aqueous and oil layers, and the distribution coefficient of each component and the equilibrium constant of the hydrolysis in both layers were calculated. It was found that the isoniazones may be classified into three types on the basis of oil/water distribution characteristics and that the calculated equilibrium constants of hydrolysis reaction in the aqueous layer coincide well with the directly measured values in aqueous solution. The distribution of isoniazone itself is so poor that the antitubercular activity of isoniazones seems to be mainly due to INAH produced by the hydrolysis reaction.抄録全体を表示PDF形式でダウンロード (479K) -
1,4-Bis〔(2-methoxy-4-propylphenoxy)acetyl〕piperazineの薬理作用入倉 勉, 西納 啓吾, 一関 紀子1963 年 83 巻 8 号 p. 785-791
発行日: 1963/08/25
公開日: 2010/02/19
ジャーナル フリーExaminations were made on the analgesic and related pharmacological action of 1, 4-bis[(2-methoxy-4-propylphenoxy)acetyl] piperazine (AP-2). Its analgesic action is equal to that of codeine phosphate by the pressure method and about one-half of that by the D'Amour-Smith method, being over 4 times that of sulpyrine. This analgesic action of AP-2 is not antagonized by nalorphine. Acute toxicity is low and there is no effect on the growth, fertility, blood picture, or tissue pattern of the organs by longterm administration. AP-2 markedly lowers the body temperature of albino rats and its antipyretic action on febrile rabbit is slightly stronger than that of sulpyrine. AP-2 has 1/2 to 1/4 of the antiphlogistic action of anlinopyrine and shows suppressive action of long duration on dextran edema and egg-white edema. It is synergistic with the hypnotic action of methylhexabital but has weak action of extending sleep. AP-2 does not antagonize convulsion caused by convulsion-producing agent.抄録全体を表示PDF形式でダウンロード (1012K) -
α-およびβ-ナフトールと2,4-ジニトロフェニルヒドラジンとの反応成績体について梅田 益雄1963 年 83 巻 8 号 p. 792-795
発行日: 1963/08/25
公開日: 2010/02/19
ジャーナル フリーIn the presence of chloramine T, the reaction between 2, 4-dinitrophenylhydrazine, and α-, β-naphthol in acidic solution afforded the corresponding products. α-Naphthol gave red needles, m. p. 277.5°(decomp.), which showed yellowish orange coloration (λmax 460mμ) in acidic solution and blue coloration (λmax 640mμ) in alkaline medium, which is reversible of having isosbestic point at 508 mμ. The elemental analysis, UV and IR spectra of the crystals are quite identical with 4-(2, 4-dinitrophenylazo)-1-naphthol which was synthesized from the reactions of α-naphthoquinone and 2, 4-dinitrophenylhydrazine or of α-naphthol and 2, 4-dinitrophenyldiazoniumsulfate. On the other hand, β-naphthol gave reddish orange needles, m. p. 305.5°(decomp.), showing orange-yellow coloration (λmax 480mμ) in acidic solution and blue (λmax 600mμ) in alkaline medium. This coloration is reversible of having isosbestic point at 522mμ. The elemental analysis, UV and IR spectra are identical with 1-(2, 4-dinitrophenylazo)-2-naphthol which was synthesized from β-naphthol and 2, 4-dinitrophenyldiazoniumsulfate but was not identical with 2-(2, 4-dinitrophenylazo)-1-naphthol which was synthesized from β-naphthoquinone and 2, 4-dinitrophenylhydrazine. Therefore, the products in this reaction were found to be 4-(2, 4-dinitrophenylazo)-1-naphthol in the case of α-naphthol and 1-(2, 4-dinitrophenylazo)-2-naphthol from β-naphthol.抄録全体を表示PDF形式でダウンロード (594K) -
高取 吉太郎, 高島 睦雄1963 年 83 巻 8 号 p. 795-799
発行日: 1963/08/25
公開日: 2010/02/19
ジャーナル フリーApplication of oxalyl chloride to 5-methoxyindole gave 5-methoxyindole-3-glyoxylyl chloride as orange-red crystals, m. p. 134°(decomp.), and application of ammonia to this chloride afforded 5-methoxyindole-3-glyoxylamide as yellow plates, m. p. 248°. The yield was almost quantitative in both reactions. Reduction of this amide with lithium aluminum hydride in a mixture of tetrahydrofuran and ether gave 5-methoxytryptamine in a good yield. Condensation of 5-methoxytryptamine and phenyl acetate by heating in tetraline or α-methylnaphthalene at 160-180° for 2 hours resulted in the formation of melatonin, obtained by Lerner and collaborators from ox pineal gland. The synthetic melatonin, obtained in a good yield, came as pale yellow leaflets, m. p. 116°, and its solution exhibited a marked yellowish green fluorescence. This substance shows absorption maximum at 277.5mμ in its ultraviolet spectrum and exhibits green by Keller's reaction and violet by van Urk's reaction, which are the specific color reactions of tryptamine series compounds.抄録全体を表示PDF形式でダウンロード (710K) -
ヒトツバハギよりDihydrosecurinineの単離斎藤 清一, 重松 暹, 堀井 善一1963 年 83 巻 8 号 p. 800-801
発行日: 1963/08/25
公開日: 2010/02/19
ジャーナル フリーA new alkaloid, m. p. 58-60°, was isolated from Securinega suffruticosa (PALL.) REHD. The minor alkaloid was identical with dihydrosecurinine which was derived chemically from securinine, the main alkaloid of the same plant.抄録全体を表示PDF形式でダウンロード (292K) -
吉岡 一郎, 山田 安広1963 年 83 巻 8 号 p. 801-802
発行日: 1963/08/25
公開日: 2010/02/19
ジャーナル フリーExtraction of the root of Inula helenium L. afforded, besides the known alantolactone-series compound, dammaradienyl acetate.抄録全体を表示PDF形式でダウンロード (312K) -
The Metalation Product of Dibenzo-p-dioxin上田 伸一1963 年 83 巻 8 号 p. 802-804
発行日: 1963/08/25
公開日: 2010/02/19
ジャーナル フリーDibenzo-p-dioxin-dicarboxylic acid derived from the dimetalation product of dibenzo-p-dioxin (I) was proved to be dibenzo-p-dioxin-1, 6-dicarboxylic acid (IV) and this proved that the metalation took place in the 1- and 6-positions of dibenzo-p-dioxin (I).抄録全体を表示PDF形式でダウンロード (418K) -
Octamethyldibenzo-p-dioxinの合成上田 伸一1963 年 83 巻 8 号 p. 805-807
発行日: 1963/08/25
公開日: 2010/02/19
ジャーナル フリーOctahalodibenzo-p-dioxin (VII) and (VIII), synthesized earlier, are negative to the dibenzo-p-dioxin reaction using conc. sulfuric acid and potassium nitrate or other oxidation agents. In order to examine whether this negative coloration is due substitution of all hydrogen atoms in the benzene ring of the octahalo derivatives with halogen atoms or to insolubility of such substance in conc. sulfuric acid, 4, 9-diethyl-1, 2, 3, 6, 7, 8-hexamethoxydibenzo-p-dioxin (IX) was synthesized and its dibenzo-p-dioxin reaction was examined. In the present series of work, octamethyldibenzo-p-dioxin (V) was synthesized by the route shown in Chart 1 and this compound was found to color blue to conc. sulfuric acid and potassium nitrate. This has shown that the presence or absence of hydrogen atoms in the dibenzo-p-dioxin skeleton does not affect the dibenzo-p-dioxin reaction.抄録全体を表示PDF形式でダウンロード (549K) -
3-Chlorocoumarilaldehyde誘導体の合成ならびにその抗白癬菌作用安茂 寿夫, 鶴田 善弘, 伊藤 昭三, 野田 克巳1963 年 83 巻 8 号 p. 807-810
発行日: 1963/08/25
公開日: 2010/02/19
ジャーナル フリーVilsmer reaction of coumaranone and its 5-chloro derivative afforded 3-chlorocoumarinaldehyde and 3, 5-dichlorocoumarinaldehyde. Condensation of these coumarin-aldehyde with various amino compounds gave the derivatives listed in Table I. In vitro test of these derivatives against Trichophyton showed results summarized in Table II.抄録全体を表示PDF形式でダウンロード (520K) -
1-ニトロソ-2-ナフトールによるモルフィンの比色定量法桜井 寛, 加藤 寿吉, 梅田 益雄, 坪田 滋基1963 年 83 巻 8 号 p. 811-814
発行日: 1963/08/25
公開日: 2010/02/19
ジャーナル フリーWhen 1-nitroso-2-naphthol and potassium nitrate were reacted with morphine in acetic acid medium in the presence of a trace of sodium nitrite, a stable coloration was observed. This reaction was adopted to the colorlmetric determination of morphine. Morphine is able to be determined without any influence, even if five times as much codeine, thebaine, narcotine and papaverine as morphine exist, but meconic acid present in opium disturbs the determination in not less than the equi-amount.
Manipulation: one ml. of the sample (morphine hydrochloride, anhydrous, 50-400μg/ml.) was taken into 10ml. graduated cylinder, 5ml. of 60mg.% of 1-nitroso-2-naphthol in acetic acid and 2ml. of 10% potassium nitrate were added and maintain at 25° for 10 min. Then, one ml. of 20mg.% sodium nitrite was added, water was later added to make 10ml. It was shaken well and kept standing at 25° for 60 min. The optical density was measured at 530mμ. The optical density was measured at 530mμ. The blank was made with water, instead of the sample.抄録全体を表示PDF形式でダウンロード (536K) -
1-ニトロソ-2-ナフトールによるオキシモルフォンの比色定量法加藤 寿吉, 佐藤 和男, 津田 健1963 年 83 巻 8 号 p. 815-817
発行日: 1963/08/25
公開日: 2010/02/19
ジャーナル フリーThe colorimetric determination of oxymorphone hydrochloride with 1-nitroso-2-naphthol and potassium nitrate was examined. As an acidic reagent hydrochloric acid was preferable instead of acetic acid used in the determination of morphine. This method follows the Beer's law within the concentration of 50-300μg./ml., and an accuracy of the measurement was σ=0.58% (n=6).
Manipulation: To one ml. of the sample (contains 50-300μg./ml., as an anhydrous oxymorphine hydrochloride), 0.5ml. of 0.04% 1-nitroso-2-naphthol was shaken and 2ml. of 15% hydrochloric acid and 1ml. of sodium nitrate added 30% potassium nitrate (0.01% sodium nitrate 0.6ml.+30% potassium nitrate 100ml.) were added. It was maintained at 25° for 10 min. Later, water was added to make 5ml. and the optical density was measured at 530mμ.抄録全体を表示PDF形式でダウンロード (465K)
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