巻号一覧
84 巻, 6 号
選択された号の論文の28件中1～28を表示しています
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1(2H)-Phthalazone類のニトロ化について金原 三郎1964 年 84 巻 6 号 p. 483-489
発行日: 1964/06/25
公開日: 2010/02/19
ジャーナル フリーNitration of 1(2H)-phthalazone (XIV) and its 4-substituted derivatives was carried out with potassium nitrate and conc. sulfuric acid. XIV formed 5-nitro compound and a minute amount of 8-nitro compound. 4-Methyl-1(2H)-phthalazone (I) chiefly formed 8-nitro compound and a small amount of 5-nitro compound. Nitration of 4-oxo-3, 4-dihydro-1-phthalazinecarboxylic acid (XXII) in the cold gave 8- and 6-nitro compounds while nitration of XXII with heating gave 6-nitro compound and decarboxylated 4, 5-dinitro-1(2H)-phthalazone (XXVIII), which is also obtained by further nitration of 5-nitro-1(2H)-phthalazone (XV) and 5-nitro-4-oxo-3, 4-dihydro-1-phthalazinecarboxylic acid (XIX). The position of nitro group in the above compounds was determined by comparison and identification with the corresponding compounds synthesized by another route (cf. Charts 1-3).抄録全体を表示PDF形式でダウンロード (1268K) -
Phthalazine類のニトロ化について金原 三郎1964 年 84 巻 6 号 p. 489-493
発行日: 1964/06/25
公開日: 2010/02/19
ジャーナル フリーNitration of phthalazine, 1-methylphthalazine, and 1-methoxyphthalazine was carried out with potassium nitrate and conc. sulfuric acid, and following results were obtained.
1) Phthalazine (I) afforded 5-nitrophthalazine (II) as the main product, with 5-nitro-1(2H)-phthalazone (III) as the by-product. II forms two kinds of methiodide and their oxidation respectively gave 2-methyl-5-nitro-1(2H)-phthalazone (VII) and 2-methyl-6-nitro-1(2H)-phthalazone (VIII).
2) 1-Methylphthalazine (X) formed 1-methyl-5-nitrophthalazine (XI) with 4-methyl-8-nitro-1(2H)-phthalazone (XII) as a by-product. Oxidation of 5-nitro-1, 3-dimethylphthala-zinium iodide (XIII), formed from XI, gave 8-nitro-2, 4-dimethyl-1(2H)-phthalazone (XV).
3) 1-Methoxyphthalazine (XVI) formed 1-methoxy-5-nitrophthalazine (XVII) with 5-nitro-1(2H)-phthalazone (XVIII) as a by-product.抄録全体を表示PDF形式でダウンロード (865K) -
1,2-Benzisothiazoline 1,1-Dioxide類の合成新田 義博, 新藤 実, 高須 哲雄, 磯野 千冬1964 年 84 巻 6 号 p. 493-497
発行日: 1964/06/25
公開日: 2010/02/19
ジャーナル フリーChlorosulfonation of 3-chlorobenzylamine hydrochloride with chlorosulfonic acid gives two kinds of labile products (II and V). Treatment of these two products with ammonia gives 5-chloro-1, 2-benzisothiazoline 1, 1-dioxide (III) from II and 5-chloro-1, 2-benzisothiazoline-6-sulfonamide 1, 1-dioxide (VI) from V. Reduction of III gives 1, 2-benzisothiazoline 1, 1-dioxide (VII) whose oxidation with potassium permanganate gives saccharine. Similar oxidation of III gives 5-chlorosaccharin (IX). The structure of III was confirmed from these experiments. Infrared spectra of these compounds were measured. III and VI showed diuretic action in mice.抄録全体を表示PDF形式でダウンロード (804K) -
Aminomethylbenzenesulfonamide類の合成新田 義博, 新藤 実, 藤森 東一, 磯野 千冬1964 年 84 巻 6 号 p. 498-503
発行日: 1964/06/25
公開日: 2010/02/19
ジャーナル フリーChlorosulfonation of N-(3-chlorobenzyl)acetamide (I), followed by ammonolysis of its product gives 2-acetamidomethyl-4-chlorobenzenesulf onamide (III) and hydrolysis of III with hydrochloric acid gives 2-aminomethyl-4-chlorobenzenesulf onamide hydrochloride (IV). Fusion of IV with the free base (V) results in cyclization to form 5-chloro-1, 2-benzisothiazoline 1, 1-dioxide (VI), which is the new compound reported in the preceding paper and the position of the chlorosulfonation is now determined. o-Aminomethylbenzenesulfonamide hydrochloride (VII) and its free base (VIII) are obtained by the catalytic reduction of IV over 10% palladium-carbon. Reaction of V and ethyl orthoformate gives 7-chloro-2, 5-dihydro-1, 2, 4-benzothiadiazepine 1, 1-dioxide (IX).
On the other hand, sulfamylation of N-(4-chlorobenzyl)acetamide (X) gives 5-acetamidomethyl-2-chlorobenzenesulfonamide (XII), which is converted to 5-aminomethyl-2-chlorobenzenesulfonamide hydrochloride (XIII) and its free base (XIV). Similar reaction of N-(2-chlorobenzyl)acetamide (XXI) gives 3-acetamidomethyl-4-chlorobenzenesulfonamide (XXIII), 3-aminomethyl-4-chlorobenzenesulfonamide hydrochloride (XXIV), and its free base (XXV). Oxidation of XIV and XXV gives the corresponding benzoic acid derivatives (XV and XXVI) which were identified.
It is concluded from these experiments that the chlorosulfonation of chlorobenzylamines is dependent on the orienting effect of the chlorine atom and not to that of the aminomethyl group. XIII. and XIV showed a fairly strong diuretic action in rats.抄録全体を表示PDF形式でダウンロード (918K) -
梅本 進1964 年 84 巻 6 号 p. 504-508
発行日: 1964/06/25
公開日: 2010/02/19
ジャーナル フリーIn order to test anti-convulsant action, ethoxycarbonylhydantoins were synthesized from the sodium salt of hydantoins and ethyl chloroformate. It was found during this synthesis that treatment of 3-ethoxycarbonyl derivatives of 5, 5-diphenyl-, 5-ethyl-5-phenyl-, 5, 5-dimethyl-, and 5-benzyl-hydantoins with sodium hydride resulted in the rearrangement of ethoxycarbonyl group to 1-position but no such rearrangement occurred in 3-ethoxycarbonyl-5-benzylidenehydantoin.抄録全体を表示PDF形式でダウンロード (734K) -
梅本 進1964 年 84 巻 6 号 p. 509-512
発行日: 1964/06/25
公開日: 2010/02/19
ジャーナル フリー3-Acylhydantoins were prepared from hydantoins and their rearrangement reaction with sodium hydride was examined. 3-Acetyl-, 3-phenylacetyl-, and 3-benzoyl-5, 5-diphenylhydantoins, and 3-acetyl derivatives of 5-ethyl-5-phenyl-, 5, 5-dimethyl-, and 5-benzyl-hydantoins underwent rearrangement with sodium hydride to give their corresponding 1-substituted derivatives but not 3-acetyl-5-benzylidenehydantoin.抄録全体を表示PDF形式でダウンロード (573K) -
島村 芳三, 三宅 良一1964 年 84 巻 6 号 p. 512-516
発行日: 1964/06/25
公開日: 2010/02/19
ジャーナル フリーThe report that Cu⋅Cr-O catalyst hydrogenated higher unsaturated acids of whale oil and other fats to the point of oleic acid series acids at 180° under atmospheric pressure was confirmed by prolongation of working period with Tsubaki oil which consists mainly of oleic acid.
Allowable high temperatures to preserve this selectivity were determined by volumetric and bubbling procedures, leading to the same conclusions that oleic acid series acids were subjected, though very slowly, to saturation at 230°, while a reduction of carboxylic group started at 260°, along with complete saturation of carbon-carbon double bond, both at minor but fairly appreciable rates.抄録全体を表示PDF形式でダウンロード (788K) -
スルファミン類と血清アルブミンとの結合の機構について中垣 正幸, 古賀 直文, 寺田 弘1964 年 84 巻 6 号 p. 516-521
発行日: 1964/06/25
公開日: 2010/02/19
ジャーナル フリーThe binding ability of crystalline bovine serum albumin was examined with several commonly used sulfonamides; sulfisomidine, sulfathiazole, sulfadimethoxine, sulfaphenazole and sulfisoxazole. The relationship between the amount of sulfonamides bound to bovine serum albumin and concentration of the sulfonamide solution at equilibrium is represented by a Langmuir-type equation. In order to study its mechanism, the binding of sulfamonomethoxine with bovine serum albumin was further examined, and in comparison with that of sulfadimethoxine, the effect of methoxyl group on the binding was discussed. Then the relationship between the charge of bovine serum albumin and its binding capacity for these six sulfonamides was examined and the standard binding affinity of sulfonamides was estimated to be about 6kcal/mole. It was concluded that in the binding of the albumin with sulfonamide, electrostatic force is the most important factor and the dissociation constant of sulfonamide affects the binding.抄録全体を表示PDF形式でダウンロード (790K) -
百瀬 勉1964 年 84 巻 6 号 p. 521-525
発行日: 1964/06/25
公開日: 2010/02/19
ジャーナル フリーAn air-bath melting point apparatus (Figs. 1, 2) was designed in which an uniform temperature was maintained with electrically heated nichrome wires and a rotating fan. The rise in temperature was easily controled with a heater by turning the dial of bimetal regulator, which was set in the furnace and operated from a room temperature to 300°.
The sample packed in a capillary tube was placed close to the horizontal side of the mercury bulb of a thermometer, and heated intermittently by turning the dial of regulator in such a way as to cause a rise in temperature of 0.5-1° per one turning in the neighborhood of the melting point, using the heater 1 for a room temperature to 100°, 2 for 100-150°, 3 for 150-200°, 4 for 200-250°, and 5 for 250-300° (Fig. 3). A preliminary heating or cooling of the furnace was very rapid as shown in the figure. The repeated determination of the melting point of several compounds (Table I) proved that the apparatus was precise enough for the usual purpose of determination.抄録全体を表示PDF形式でダウンロード (1241K) -
百瀬 勉, 大倉 洋甫, 小橋 一弥, 矢野 良子, 大橋 勝子, 永田 礼子, 太田 紀代子1964 年 84 巻 6 号 p. 525-531
発行日: 1964/06/25
公開日: 2010/02/19
ジャーナル フリーSodium tungustate and alum was used for the deproteinization of diluted serum to determine creatinine and creatine with picric acid or 1, 3, 5-trinitrobenzene as the color developing agent. Sulfamic acid proved to be suitable for the conversion of creatine to creatinine in a simple procedure.
These methods of determination give the creatinine and creatine values analogous to those determined by the Folin-Wu method. Precision of the methods is shown in the tables.抄録全体を表示PDF形式でダウンロード (823K) -
Bisbenzylisoquinoline Alkaloidsの合成研究 (第1報) dl-3-Amino-3´-methoxy-4,4´-bis (2-methyl-6,7-dimethoxy-1,2,3,4-tetrahydro-1-isoquinolylmethyl) diphenyl Etherの合成亀谷 哲治, 福本 圭一郎, 呂 政府1964 年 84 巻 6 号 p. 532-537
発行日: 1964/06/25
公開日: 2010/02/19
ジャーナル フリーAztequine (I), m.p. 176°, is an alkaloid isolated in 1948 by Pallares and Garza from the leaves of a Mexican Magnoliaceae plant, yoloxochitl (Talauma mexicana DON.). As a preliminary to the total synthesis of I, synthesis of tetramethylaztequine (II) was attempted. In general, presence of an electron-attracting group like nitro in the position ortho or para to the halogen results in smooth progress of the Ullmann reaction, with a good yield. Therefore, 3-nitro-4-bromobenzaldehyde, obtained by nitration of 4-bromobenzaldehyde, and vanillin were submitted to the Ullmann reaction and 3-nitro-4-(2-methoxy-4-formylphenoxy)-benzaldehyed was obtained. Its reduction with sodium borohydride to the dialcohol, followed by chlorination and derivation to the dinitrile, and hydrolysis with conc. hydrochloric acid afforded the objective dihomo acid. Its fusion with homoveratrylamine or its Schotten-Baumann reaction gave the corresponding diamide (XXVII) whose Bischler-Napieralski reaction produced bis (3, 4-dihydroisoquinoline) derivative. Catalytic reduction of its methiodide (XXIX) finally afforded rac-3-amino-3′-methoxy-4, 4′-bis (2-methyl-6, 7-dimethoxy-1, 2, 3, 4-tetrahydro-1-isoquinolylmethyl)-diphenyl ether (XXXI). Attempt to diazotize XXXI to change the amino group into hydroxyl and its methylation to obtain II did not materialize.抄録全体を表示PDF形式でダウンロード (1055K) -
ニトロフラン誘導体の化学構造と抗ガン作用との関係について三浦 孝次, 池田 政男, 大橋 富次, 岡田 いく子, 五十嵐 良子1964 年 84 巻 6 号 p. 537-543
発行日: 1964/06/25
公開日: 2010/02/19
ジャーナル フリーEffect of 2-[2-(5-nitro-2-furyl) vinyl] quinoline (2-Q-ran) and 17 other compounds on mice bearing Ehrlich ascites tumor was examined. 2-Q-ran was found to have a marked antitumor action and its intraperitoneal administration in a suitable dose effected 50-day prolongation of life in all the test animals and avoided them from tumor death.
Effect of the side chain on antitumor activity was then examined and it was found that the compounds having N-oxide, carbonamide, or two amino groups showed approximately the same effect as the parent compound and that the nitro, bromo, and acetamide groups gave a marked effect in decreasing the antitumor activity.
Panfuran having an as-triazine and T-ran having a thiadiazole ring were both ineffective but X-ran having a quinoxaline ring had an effect comparable to that of 2-Q-ran.
In order to elucidate the action mechanism of nitrofurylvinylquinoline derivatives, their effect on the nucleic acid and protein syntheses by Escherichia coli was examined. and it was found that the nitrofuran systems having antitumor action strongly inhibited biosynthesis of deoxyribonucleic acid, ribonucleic acid, and proteins. 4, 6-Diamino-2-Q-ran was found to inhibit ascites tumor dehydrogenase. It may be concluded that these nitrofuran derivatives show their antitumor action as the cytotoxic substance in a wide sense.抄録全体を表示PDF形式でダウンロード (968K) -
アミノ酸類とTetramethylpyrazine生成との関係足立 多平, 神谷 弘子, 小菅 卓夫1964 年 84 巻 6 号 p. 543-545
発行日: 1964/06/25
公開日: 2010/02/19
ジャーナル フリーTetramethylpyrazine was first produced by Bacillus subtilis in a medium having asparagine as the sole source of nitrogen. It was found that it is also produced when aspartic acid, alanine, glutamic acid, arginine, or peptone is used as the sole source of nitrogen.抄録全体を表示PDF形式でダウンロード (471K) -
Tetramethylpyrazineの定量法および生成機作について足立 多平, 神谷 弘子, 小菅 卓夫1964 年 84 巻 6 号 p. 545-548
発行日: 1964/06/25
公開日: 2010/02/19
ジャーナル フリーAs a method for detection of tetramethylpyrazine, use of ultraviolet spectrum was examined. It was assumed that acetoin would be formed as a precursur of tetramethyl-pyrazine from the result of shake culture and a mechanism was presumed for the formation of tetramethylpyrazine in a medium added with acetoin.抄録全体を表示PDF形式でダウンロード (595K) -
Tuberostemonineの脱水素反応の研究 その1上尾 庄次郎, 新宮 徹朗, 津田 喜典, 大和 譲1964 年 84 巻 6 号 p. 548-552
発行日: 1964/06/25
公開日: 2010/02/19
ジャーナル フリーThe alkaloid tuberostemonine, obtained from Stemona tuberosa L., was dehydrogenated over 40% palladium-asbestos to give, along with small amounts of three crystalline compounds, tuberostemonane, C20H29N, as an oil, the yield of which was raised to 70% by the use of 20% palladium-charcoal as a catalyst under selected conditions. Oxidation of tuberostemonane with chromium trioxide-pyridine complex or with potassium permanganate afforded an orange-red substance, C16H19O2N, whose ultraviolet and infrared spectra indicated that it is an isatin, suggesting that tuberostemonane possesses an indole skeleton.抄録全体を表示PDF形式でダウンロード (1019K) -
Tuberostemonineの脱水素反応の研究 その2上尾 庄次郎, 新宮 徹朗1964 年 84 巻 6 号 p. 552-555
発行日: 1964/06/25
公開日: 2010/02/19
ジャーナル フリーComparative dehydrogenation studies on the relationship between the catalyst and the product from tuberostemonine revealed that crystalline dehydrogenation products rather than oily tuberostemonane can best be obtained by the use of a palladium-asbestos catalyst containing a trace of sodium carbonate.抄録全体を表示PDF形式でダウンロード (814K) -
Tuberostemonaneの構造上尾 庄次郎, 新宮 徹朗1964 年 84 巻 6 号 p. 555-561
発行日: 1964/06/25
公開日: 2010/02/19
ジャーナル フリーBased on degradative and synthetic investigations, the structure of tuberostemonane, a dehydrogenation product of the alkaloid tuberostemonine, has been shown to be represented by the formula (IX).抄録全体を表示PDF形式でダウンロード (1156K) -
(+)-チオクト酸アミドの合成出口 義雄, 三浦 一子1964 年 84 巻 6 号 p. 562-563
発行日: 1964/06/25
公開日: 2010/02/19
ジャーナル フリーLevorotatory thioctic acid has biological, activity and the compound has already been synthesized. (+)-Thioctamide was synthesized from (+)-6, 8-dichloroöctanoic acid (I) by the method already reported, using sodium disulfide. Its activity tested by Streptococcus faecalis 10Cl is about twice that of the racemic compound.抄録全体を表示PDF形式でダウンロード (322K) -
サイクラミン酸ナトリウムの比色定量における呈色色素について市川 正孝, 児島 昭次, 一番ケ瀬 尚1964 年 84 巻 6 号 p. 563-566
発行日: 1964/06/25
公開日: 2010/02/19
ジャーナル フリーSodium cyclamate (sodium N-cyclohexanesulfamate) is hydrolyzed in hydrochloric acid, in the presence of hydrogen peroxide, and forms cyclohexylamine. When the concentration of cyclohexylamine in the hydrolysis solution was less than 0.025%, the amine was extracted with chloroform, ethanolic solution of quinhydrone was added to it, and the mixture was warmed at 50° for 2 hours, giving cyclohexylamino-1, 4-benzoquinone (I), m. p. 96-98°. I was also obtained by the use of 1, 4-benzoquinone in place of quinhydrone.
When the concentration of cyclohexylamine was over 0.25%, excess of manganese dioxide was added to the hydrolysis solution to decompose hydrogen peroxide, the solution adjusted to pH 9.0 with a buffer solution, and ethanolic solution of quinhydrone was added. The mixture was warmed at 50° for 15 minutes, and extracted with chloroform in hydrochloric acidity, by which 2, 5-bis(cyclohexylamino)-1, 4-benzoquinone (II), m. p. 242°, was obtained. II was also obtained by refluxing 2, 5-dimethoxy-1, 4-benzoquinone and cyclohexylamine in ethanol. I and II were identified as the colored substances obtained in the quinhydrone method for identification of sodium cyclomate.抄録全体を表示PDF形式でダウンロード (601K) -
3-Methylthio-4-alkyl-5-[2-(5-nitro-2-furyl)vinyl]-1,2,4-triazoleの合成才川 勇1964 年 84 巻 6 号 p. 566-569
発行日: 1964/06/25
公開日: 2010/02/19
ジャーナル フリーReaction condition for cyclization of 1-[3-(5-nitro-2-furyl)acryloyl]-4-alkyl-S-methylisothiosemicarbazides (I) leading to 3-methylthio-4-alkyl-5-[2-(5-nitro-2-furyl)vinyl]-1, 2, 4-triazoles (III), was examined. The best method for preparing III was found to be boiling of dioxane solution of I in the presence of an organic acid or a base like acetic acid or piperidine. Physical properties of III are shown in Table I.抄録全体を表示PDF形式でダウンロード (496K) -
山名 月中, 水上 勇三, 市村 藤雄, 古池 宏, 本谷 千枝1964 年 84 巻 6 号 p. 570
発行日: 1964/06/25
公開日: 2010/02/19
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1964 年 84 巻 6 号 p. e1a
発行日: 1964年
公開日: 2010/02/19
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1964 年 84 巻 6 号 p. e1b
発行日: 1964年
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1964 年 84 巻 6 号 p. e1c
発行日: 1964年
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1964 年 84 巻 6 号 p. e1d
発行日: 1964年
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1964 年 84 巻 6 号 p. e1e
発行日: 1964年
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1964 年 84 巻 6 号 p. e1f
発行日: 1964年
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1964 年 84 巻 6 号 p. e1g
発行日: 1964年
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