巻号一覧
84 巻, 2 号
選択された号の論文の17件中1～17を表示しています
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鈴木 真言1964 年 84 巻 2 号 p. 95-108
発行日: 1964/02/25
公開日: 2010/02/19
ジャーナル フリーPDF形式でダウンロード (2289K) -
3-Amino-5,6-dimethyl-1,2,4-triazineとアルデヒド類との縮合生成物について才川 勇, 高井 明, 児玉 寛1964 年 84 巻 2 号 p. 109-114
発行日: 1964/02/25
公開日: 2010/02/19
ジャーナル フリーReaction of 3-amino-5, 6-dimethyl-1, 2, 4-triazine (IVb) with 5-nitrofurfural, 5-nitro-2-thiophenecarboxaldehyde, and 4-nitrobenzaldehyde in the presence of sulfuric acid afforded the condensation products 5-[2-(5-nitro-2-furyl)vinyl], 5-[2-(5-nitro-2-thienyl)-vinyl], and 5-(4-nitrostyryl) derivatives of 3-amino-6-methyl-1, 2, 4-triazine, respectively.
It was suggested that condensation of IVb with arylaldehydes took place at the 5-methyl, by examination of ultraviolet spectra of the products and from a consideration of reaction mechanism. From 5-nitro-2-furanacroleins, 5-[4-(5-nitro-2-furyl)butadienyl]-3-amino-6-methyl-1, 2, 4-triazines shown in Table III were also prepared. These new compounds failed to show expected antibacterial activity (Table II).抄録全体を表示PDF形式でダウンロード (801K) -
ニトロフラン系化合物の試験管内生物学的活性における失活現象について才川 勇, 高井 明, 高道 郁子, 織田 武, 児玉 寛1964 年 84 巻 2 号 p. 115-120
発行日: 1964/02/25
公開日: 2010/02/19
ジャーナル フリー3-Amino-6-[2-(5-nitro-2-furyl)vinyl]-1, 2, 4-trlazrne (I) readily formed an adduct (III) with cysteine hydrochloride in water, whereas I gave unidentified brown crystalline mass (IV) when treated with cysteine in alkaline medium. IV failed to exhibit antibacterial activity or any specific ultraviolet absorption spectrum. Thioglycolic acid behaved similarly as cysteine with I. Antibacterial activity of I in bouillon medium was reduced to 1/200 by the addition of 0.08% cysteine at pH 8.6-9.0.
This SH-inhibition was inhibited by p-chloromercuribenzoate, mercurichloride, cupric acetate, and some quinones. Activity of I and related compounds shown in Table VI was also reduced by human serum and by cysteine.抄録全体を表示PDF形式でダウンロード (935K) -
ニトロフラン核を有する2-Aminopyrimidine類の合成および構造活性相関について才川 勇1964 年 84 巻 2 号 p. 121-130
発行日: 1964/02/25
公開日: 2010/02/19
ジャーナル フリー4-(5-Nltro-2-furylalkenyl) and 4-(5-nitro-2-thienylalkenyl) derivatives of 5-substituted 2-aminopyrimidine shown in Tables I-III were prepared. Antibacterial activity of these new compounds against Escherichia coli O-18 and Staphylococcus aureus 209P was tested in three kinds of bouillon medium and its result is summarized in Tables IV-VII. It was found that 5-substituted 2-amino-4-[3-methyl-4-(5-nitro-2-furyl)butadienyl]pyrimidines have strong antibacterial activity.抄録全体を表示PDF形式でダウンロード (1413K) -
ニトロフラン核を有する2-置換アミノピリミジン類の合成および構造活性相関について才川 勇, 前田 豊男1964 年 84 巻 2 号 p. 131-137
発行日: 1964/02/25
公開日: 2010/02/19
ジャーナル フリーReaction of 2-(substituted amino)-4-methylpyrimidines with 5-nitro-2-furyl-aldehydes and 5-nitro-2-thienyl-aldehydes afforded 2-(substituted amino)-4-(5-nitro-2-furylalkenyl)-pyrimidines (V) and 2-(substituted amino)-4-(5-nitro-2-thienylalkenyl) pyrimidines (VII), respectively.
Some N-hydroxymethyl derivatives of V were also prepared. Antibacterial activity of these new compounds against Escherichia coli O-18 and Staphylococcus aureus 209P was tested in three kinds of bouillon medium and its result is summarized in Tables IV and V. 2-Methylamino-4-[3-methyl-4-(5-nitro-2-furyl)butadienyl]pyrimidine showed strong antibacterial activity.抄録全体を表示PDF形式でダウンロード (1033K) -
Methyl (methylthio) mercuryの合成近藤 孝子1964 年 84 巻 2 号 p. 137-141
発行日: 1964/02/25
公開日: 2010/02/19
ジャーナル フリーBy passing methanethiol into an alcoholic solution of methylmercury hydroxide, a new organomercury compound was obtained. From elementary analysis, molecular weight, and infrared spectrum it was identified as methyl (methylthio) mercury.抄録全体を表示PDF形式でダウンロード (769K) -
Methyl cis- and trans-1-Methyldecahydro-3-quinolinecarboxylateの合成堀井 善一, 渡辺 利郎, 池田 正澄, 栗原 拓史, 田村 恭光1964 年 84 巻 2 号 p. 142-145
発行日: 1964/02/25
公開日: 2010/02/19
ジャーナル フリーMethods of synthesizing methyl trans-1-methyldecahydro-3-quinolinecarboxylate (VI) and its cis isomer (X, R=CH3) were investigated. Sodium borohydride reduction and dehydration converted ethyl trans-1-methyl-4-oxodecahydro-3-quinolinecarboxylate (I) to 1-methyl-1, 2, 4a, 5, 6, 7, 8, 8a-octahydro-3-quinolinecarboxylic acid (III). Catalytic reduction and subsequent esterification of III yielded the trans compound (VI). The cis compound (X, R=CH3) was synthesized by condensation of cyclohexanone and ethyl 2-(methylaminomethyl)acrylate followed by catalytic reduction. Catalytic reduction of methyl 3-quinolinecarboxylate (VII) followed by N-methylation gave VI as a major product and X, R=CH3 as a minor product.抄録全体を表示PDF形式でダウンロード (725K) -
13-Oxo誘導体の合成と反応 (補遺)近藤 嘉和1964 年 84 巻 2 号 p. 146-151
発行日: 1964/02/25
公開日: 2010/02/19
ジャーナル フリーThe product obtained by oxidation of 8-acetonyldihydroberberine (II) with potassium permanganate, corresponding to the molecular formula of C23H25O6N, UV λmax 286mμ (log ε3.78), νOH 3420 cm-1 (KBr), was acetylated to a monoacetate, m. p. 256.5-257°. Its structural formula as represented by IIIb and IIIc was denied from its absorption maximum at 287mμ (log ε 3.83) and the previously proposed formula of IIIa was proved to be the most appropriate. Reduction of IIIa with sodium borohydride in ethanol afforded 8-(2-hydroxypropyl)-13-acetoxy-2, 3-methylenedioxy-9, 10-dimethoxy-dibenzo[a, g]quinolizidine (VII), m. p. 184°, as well as its deacetylated compound, 8-(2-hydroxypropyl)-13-hydroxy-2, 3-methylenedioxy-9, 10-dimethoxydibenzo[a, g]quinolizidine (VI) and the 2′-hydroxy epimer of VII as its acetate of m. p. 196-198°.
Reduction of the 13-methoxy compound (XV), obtained from IIIa through XIII and XIV, with sodium borohydride afforded 13-methoxy-2, 3-methylenedioxy-9, 10-dimethoxydibenzo[a, g]quinolizidine (XVI) and its demethoxylated, berberinium-type quaternary base as aby-product. Reduction of XV with lithium aluminum hydride in tetrahydrofuran resulted in demethylation to form 13-hydroxy-2, 3-methylenedioxy-9, 10-dimethoxydibenzd[a, g]quinolizidine (XVII). All these products were identified with authentic speciments. The position of the hydroxyl group in XVII was confirmed as 13-position by comparison with the methiodide of XVII and with allocryptopine hydriodide (XXIII).抄録全体を表示PDF形式でダウンロード (968K) -
非イオン活性剤ベンゼン溶液に対する水の自己乳化および可溶化過程中垣 正幸, 曾根 節子1964 年 84 巻 2 号 p. 151-155
発行日: 1964/02/25
公開日: 2010/02/19
ジャーナル フリーAutoëmulsification and solubilization process of water in benzene solution of polyoxyethylene-system nonionic surfactant were examined by layering method at 25° and it was found that autoëmulsification occurred at the zone of contact of water and oil phases, water droplets formed are dispersed into the oil layer, and then solubilized in the oil layer, excess water combining again with the aqueous phase to reach solubilization equilibrium. Amount of water solubilized in benzene solution of a surfactant increases linearly with increasing concentration of the surfactant and the amount of solubilization tended to become greater with greater average molar number of ethylene oxide added, i.e. with greater HLB value. Amount of water solubilization is independent of the kind of hydrophobic groups in the surfactant and it was found that ca. 1 mole of water is solubilized by 10 moles of ethylene oxide added. Apparent c. m. c. of poiyoxyethylene octylphenyl ether, polyoxyethylene nonylphenyl ether is almost zero but in polyoxyethylene lauryl ether, c. m. c. becomes smaller as the added moles of ethylene oxide becomes greater.抄録全体を表示PDF形式でダウンロード (831K) -
3-Phenyl-2-quinoxalinecarbonitrileについて林 英作, 飯島 千穗子1964 年 84 巻 2 号 p. 156-162
発行日: 1964/02/25
公開日: 2010/02/19
ジャーナル フリーVarious reactions of 3-phenyl-2-quinoxalinecarbonitrile (I) were examined, and the course of the reaction and reaction products are illustrated by the reaction formulae. The reactions carried out were as follows: Reaction with hydrogen peroxide in the presence of alkali or in acetic acid; reaction with monoperphthalic acid (for comparison with that with hydrogen peroxide in acetic acid); reaction with acid, alkali, sodium methoxide, Grignard reagent, and with amines.抄録全体を表示PDF形式でダウンロード (1019K) -
2位および2位と3位に置換基のあるQuinoxalineのN-Oxidationについて林 英作, 飯島 千穗子, 長沢 陽子1964 年 84 巻 2 号 p. 163-183
発行日: 1964/02/25
公開日: 2010/02/19
ジャーナル フリーQuinoxalines substituted in 2-position and in 2- and 3-positions were submitted to N-oxidation to examine the effect of adjacent substituent on the ring nitrogen. N-Oxidation was carried out with (a) monoperphthalic acid in ether or benzene at below 10° and (b) hydrogen peroxide in acetic acid at an appropriate temperature between 60 and 100°. Results of these reactions are presented in the reaction formulae and following conclusions were drawn.
1) Effect of adjacent substituent on the ring nitrogen during N-oxidation:
(i) Methyl group slightly facilitates the formation of N-oxide.
(ii) Primary alkyl groups like ethyl and propyl do not interfere in the formation of N-oxide but it is uncertain whether they facilitate the formation.
(iii) Isopropyl group (and probably secondary alkyl groups in general) have fairly great adverse effect on the formation of N-oxide
(iv) Phenyl group have some adverse effect on the formation of N-oxide but not enough to prevent its formation.
(v) Alkoxyl, chloro, cyano, carbamoyl, ethoxycarbonyl, carboxy, and acyl groups have fairly great interfering action on N-oxide formation.
(vi) When there are substituents in the 2- and 3-positions, result of the reaction cannot be predicted from the foregoing conclusions (i) to (v), and the reaction result seems to be determined in some cases by the correlation of the two substituents. For example, only the 4-oxide is formed from 2-quinoxalinecarboxamide (XXIX) and not 1-oxide or 1, 4-dioxide, while only the 1-oxide is formed from 3-phenyl-2-quinoxalinecarboxamide (LXXVII) and not 4-oxide or 1, 4-dioxide.
2) Side reactions:
(i) Alkoxy and chloro groups interfere in the formation of N-oxide but a more drastic reaction conditions in the (b) method, such as elevation of reaction temperature and prolongation of reaction time, results in the acceleration of the hydrolysis of these groups, a side reaction rather than the formation of N-oxide.
(ii) Ring carbon to which carbamoyl or aryl group is bonded undergoes oxidation, with liberation of the substituent, and sometimes results in a side reaction with subsequent substitution with hydroxy group.
(iii) When cyano group is present, treatment with monoperphthalic acid results in more facile change of chano group into carbamoyl group rather than N-oxidation. Consequently, treatment with hydrogen peroxide is more suitable than with monoperphthalic acid.抄録全体を表示PDF形式でダウンロード (3834K) -
坂井 進一郎, 原田 正敏, 森下 郁夫, 菊池 友宏1964 年 84 巻 2 号 p. 183-187
発行日: 1964/02/25
公開日: 2010/02/19
ジャーナル フリーCrude drug formulas often used call for a combination of Ephedra, Chinese cinnamon, and Japanese apricot seeds. Chemical reaction of their representative components, ephedrine, cinnamaldehyde, and benzaldehyde in their decoction is possible. From such a point, oxazolidine condensates of l- and d-pseudoephedrine and cinnamaldehyde were synthesized and their acute toxicity, relaxation of guinea-pig tracheal muscle, and effect on blood pressure and respiration of rabbits were examined. Presence of these oxazolidine condensates in the decoction was also examined.
These oxazolidine condensates are labile in polar solvents and undergo ring fission and decomposition. Consequently, such condensates were not formed in the decoction. Results of pharmacological tests are given in Table I and all were less effective than l-ephedrine, though each differing to some extent.抄録全体を表示PDF形式でダウンロード (987K) -
Thioxolone誘導体の研究豊島 昭二, 島田 勝年, 田中 悟, 金沢 保, 河部 靖1964 年 84 巻 2 号 p. 187-191
発行日: 1964/02/25
公開日: 2010/02/19
ジャーナル フリーThioxolone (4-hydroxy-2H-1, 3-benzoxathiol-2-one) and its 35 new derivatives, and two other compounds were synthesized and their in vitro antifungal activity was examined. 5-Chlorothioxolone and its acetate, propionate, and butyrate, and 5, 7-dichlorothioxolone inhibited the growth of Trichophyton and Microsporum in 3.13-6.25γ/ml. concentration, showing stronger antifungal activity than thioxolone. However, growth inhibitory action of these compounds against other fungi and bacteria was weak.抄録全体を表示PDF形式でダウンロード (716K) -
ニトロフラン誘導体の合成研究 2-(5-Nitro-2-furyl)-5-alkylthio-1,3,4-thiadiazoleの合成および抗菌作用豊島 昭二, 島田 勝年, 杉山 国重, 河部 靖1964 年 84 巻 2 号 p. 192-194
発行日: 1964/02/25
公開日: 2010/02/19
ジャーナル フリー2-(5-Nitro-2-furyl)-5-alkylthio-1, 3, 4-thiadiazole was prepared by oxidation of 5-nitro-2-furfural alkyldithiocarbohydrazone with ferric chloride or by dehydration of (5-nitro-2-furoyl)alkyl dithiocarbazate with conc. sulfuric acid. Antibacterial action of these compounds are shown in Table I.抄録全体を表示PDF形式でダウンロード (477K) -
クエルセチン3,5-ジメチルエーテル “Caryatin” およびガランギン3,5-ジメチルエーテルの合成について佐々木 豊作1964 年 84 巻 2 号 p. 195-198
発行日: 1964/02/25
公開日: 2010/02/19
ジャーナル フリーQuercetin 3, 5-dimethyl ether was synthesized by heating a mixture of 4′, 6′-dihydroxy-2, 2′-dimethoxyacetophenone, dibenzoylprotocatechuic anhydride, and potassium dibenzoylprotocatechuate at 180-185° for 3 hours by the method of Allan and Robinson. The product was obtained as a slightly yellowish crystals with a composition of C17H14O7⋅CH3OH from dehydrated methanol and of C17H14O7⋅3H2O from hydrous methanol, both melting at 299-301°. Acetate: Colorless needles, m.p. 140-142°, C17H11O7(COCH3)3 Various properties of the ether were entirely identical with those of caryatin from pecan, and no difference was found in mixed fusion test, paper partition chromatography, and absorption spectra. A considerable amount of a byproduct was obtained in the foregoing synthesis as colorless needles, m.p. 282-283°, which was identified with galangin 3, 5-dimethyl ether, m.p. 282-283°, synthesized by the Allen, Robinson method.抄録全体を表示PDF形式でダウンロード (693K) -
林 英作, 長尾 隆子1964 年 84 巻 2 号 p. 198-201
発行日: 1964/02/25
公開日: 2010/02/19
ジャーナル フリーCatalytic reduction of 1, 2, 3, 4-tetrahydroacridine (I) in methanol at ordinary temperature and pressure, with palladium-platinum-carbon as a catalyst, results in smooth progress of the reaction to form 1, 2, 3, 4, 4a, 9, 9a, 10-octahydroacridine (II). Similarly, 1, 2, 3, 4, 4a, 9, 9a, 10-octahydro-4-acridinol (IX) is formed from 1, 2, 3, 4-tetrahydro-4-acridinol (VIII) and methyl 1, 2, 3, 4, 4a, 9, 9a, 10-octahydro-9-acridinecarboxylate (XI) from methyl 1, 2, 3, 4-tetrahydro-9-acridinecarboxylate (X). Quinoline (IV), quinaldine (V), 2-ethyl-3-methylquinoline (VI), and 7, 8, 9, 10-tetrahydrophenanthridine (VII) are not reduced under these conditions. The reduction does not progress by the use of palladium-carbon or Raney nickel in place of palladium-platinum-carbon, and the reaction is markedly retarded by the use of platinum-carbon. There should be stereoisomers of II, IX, and XI, but no examinations were made on this point. The compound (II) obtained by this reaction melted at 70° and its N-acetylated compound showed m.p. 136°, which are assumed to correspond to one of the two stereoisomers separated from (II) synthesized by Perkin, et al. through a different route; the one of m.p. 82° and its N-acetylated compound of m.p. 86°, and the other of m.p. 72° and its N-acetylated compound of m.p. 136°.抄録全体を表示PDF形式でダウンロード (620K) -
長瀬 雄三, 馬場 茂雄, 井戸 達雄1964 年 84 巻 2 号 p. 202-205
発行日: 1964/02/25
公開日: 2010/02/19
ジャーナル フリーExaminations were made on the measurement of radioactivity using a liquid scintillation counter by removal of the effect of quenching action of colored nitre compounds. In this method, the sample is electrolytically reduced directly in the vessel for the measurement, hydrophilic scintillator is added, and measured at an applied voltage of 1300v. and a discriminator voltage of 10v.-∞.
This method was used on model compounds, 2, 4-dinitrophenylhydrazine derivatives of propiophenone [1-14C] and 4-methoxybenzophenone [carbonyl-14C], and measurement was made with around 90% efficiency. Reproducibility of this method was within a statistical error.抄録全体を表示PDF形式でダウンロード (461K)
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