巻号一覧
76 巻, 5 号
選択された号の論文の39件中1～39を表示しています
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松本 克, 曾根 節子1956 年 76 巻 5 号 p. 475-478
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーMutual solubility of the monoethylene glycol-water-butanol system was measured at 20° and 44°. It was thereby found that the mutual solubility became greater as the temperature became higer and that the mutual solubility at 20° was greater in the system containing butanol as compared to the system with amyl alcohol or hexyl alcohol, which was the smallest. Comparison of the distribution curves of these three systems showed the slope of the curve to be the most gentle in the system with butanol. The tie-line data of the monoethylene glycol-water-butanol system was obtained by the measurement of its refractive index.抄録全体を表示PDF形式でダウンロード (527K) -
松本 克, 曾根 節子1956 年 76 巻 5 号 p. 478-481
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーMutual solubility of the diethylene glycol-water-butanol and triethylene glycol-water-butanol systems was measured at 20° and 40°. It was thereby found that the mutual solubility of these systems increased with increase of temperature, as in the case of monoethylene glycol-water-butanol system, though the solubility itself was somewhat greater than the latter. The difference in the solubilities between the two systems was very small. Comparison of the distribution curves of these three systems showed that glycol was distributed largely in the aqueous phase, especially at low temperatures and that lower glycols were distributed in a larger amount. The tie-line data of these systems at 20° and 40° were obtained from the measurement of their refractive indices and were found to be linear.抄録全体を表示PDF形式でダウンロード (424K) -
Ethyl 3-Ethoxycarbonylpyrrole-2-acetate誘導体の合成山元 清嗣, 木村 碩志1956 年 76 巻 5 号 p. 482-485
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーCondensation of α-amino ketone, derived from α-amino acid by the Dakin-West reaction, with diethyl acetonedicarboxylate afforded five kinds of ethyl 3-ethoxy-carbonylpyrrole-2-acetate, the acetate radical at α-position in which was saponified, and five new derivatives of 3-ethoxycarbonylpyrrole-2-acetic acid were obtained. Application of diethyl oxalacetate or diethyl acetonedicarboxylate on 2-amino-4′-hydroxyacetophenone hydroiodide and 2-amino-2′, 4′-dihydroxyacetophenone hydrochloride afforded 3-ethoxycarbonyl-4-(4-hydroxyphenyl) pyrrole-2-carboxylic acid and ethyl 3-ethoxycarbonyl-4-(4-hydroxyphenyl) pyrrole-2-acetate from the former reacting with both keto acid esters, while the latter only reacted with diethyl acetonedicarboxylate and afforded ethyl 3-ethoxycarbonyl-4-(2, 4-dihydroxyphenyl)-pyrrole-2-acetate.抄録全体を表示PDF形式でダウンロード (850K) -
Ethyl 2-Ethoxycarbonylpyrrole-3-acetate誘導体の合成山元 清嗣1956 年 76 巻 5 号 p. 485-488
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーBy submitting acetylacetone and oximino-acetonedicarboxylic ester (I) to Knorr synthesis, a new derivative (III) was obtained and was derived to (IV) by catalytic reduction with platinum oxide. The so-called sulfuryl chloride reaction on (IV) resulted in the oxidation of the methyl group in the 5-position of ethyl 2-ethoxycarbonylpyrrole-3-acetate to the aldehyde and (V) was obtained in a good yield. Further, the aldehyde group was oxidized to the carboxyl, which was then changed to bromine by the action of bromine to (VII). Reduction of the aldehyde group in (V) with sodium borohydride afforded dipyrrylmethane (XIII) and not the corresponding carbinol. Saponification of the ethyl 2-ethoxycarbonylpyrrole-3-acetate derivatives showed that the ethyl acetate radical in the 3-position of (IV) and (VII) is more easily saponified than the ethoxycarbonyl group in the 2-position, while the compound (III) possessing an acetyl group in the 4-position was saponified at the both ester groups and formed (VIII).抄録全体を表示PDF形式でダウンロード (762K) -
サントニン関連化合物のC6水酸化法I 数種のDihydrosantonin異性体の合成石川 尚1956 年 76 巻 5 号 p. 489-494
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーTreatment of the enol acetate (III) of methyl 3-oxo-11-epi-isoeusanton-4-enate (II) with organic peracid affords trans-hydroxy ester (IV) with the hydroxyl group introduced into C6β-position and its bromination-dehydrobromination to the methyl santoninate isomer followed by saponification results in the reversion of the hydroxyl at C6 to form rac-6α-hydroxy-3-oxo-11-epi-isoeusantona-1, 4-dienic acid lactone (VII), or rac-santonin A. Treatment of the enol acetate (XIII) of methyl 3-oxoeusanton-4-enate (XII) with performic acid produces 6α-hydroxy-3-oxoeusanton-4-enic acid lactone (XIV), or dihydro-α-santonin, and 6β-hydroxy lactone (XV), or dihydrosantonin C, while the same treatment of methyl 3-oxo-11-epi-eusanton-4-enate (XVI) affords 6α-hydroxy-3-oxo-11-epi-eusanton-4-enic acid lactone (XVIII), or dihydro-β-santonin, and 6β-hydroxy lactone (XIX), or dihydrosantonin D. Treatment of the C6-Br compound (VIII), obtained as the main product from the Wohl-Ziegler reaction of (II), with sodium iodide gives the trans-hydroxy ester (IV) and the treatment of (VIII) with anhydrous silver oxide gives the cis-hydroxy ester (X), suggesting an α-configuration for the foregoing C6-bromine.抄録全体を表示PDF形式でダウンロード (1247K) -
サントニン関連化合物のC6水酸化法II 11-Norsantoninおよびその異性体の合成石川 尚1956 年 76 巻 5 号 p. 494-500
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーTreatment of the enol acetate (II) of ethyl 11-ethoxycarbonyl-3-oxo-11-noreusanton-4-enate (I) with performic acid results, on one hand, in the introduction of a hydroxyl group in cis-form and formation of the lactonized 11-ethoxycarbonyl-6β-hydroxy-3-oxo-11-epi-11-noreusanton-4-enic acid lactone (III), and on the other, in formylation with the introduction of a hydroxyl group in trans-form, without lactonization, and formation of ethyl 11-ethoxycarbonyl-6α-formyloxy-3-oxo-11-noreusanton-4-enate (VIII), in approximately the same amount. Later treatment of (VIII) produces rac-11-norsantonin (XVI), with a trans-lactone ring, and (III), its isomer (VII) with a cis-lactone ring. Optically active compound of 11-norsan-tonin (XVI) was also synthesized.抄録全体を表示PDF形式でダウンロード (1254K) -
6β-Hydroxy-3-oxo-11-epi-eusantona-1,4-dienic Acid Lactone (Santonin D)の合成別法石川 尚1956 年 76 巻 5 号 p. 500-504
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーPartial saponification of ethyl 11-ethoxycarbonyl-3-oxoeusanton-4-enate (I) produces two kinds of monoesters (II and XII), which are epimers at C11-position. Bromination-dehydrobromination of these esters affords the corresponding dienonelactonic esters (V and XV) and their saponification followed by decarboxylation give, from both, 6β-hydroxy-3-oxo-11-epi-eusantona-1, 4-dienic acid lactone (XI) or rac-santonin D, which is also obtained by the bromination-dehydrobromination of 11-carboxy-3-oxoeusanton-4-enic acid (XVI).抄録全体を表示PDF形式でダウンロード (985K) -
サントニンの新転位反応I 天然産サントニンの転位石川 尚1956 年 76 巻 5 号 p. 504-507
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーWarming of l-α-santonin (Ia) with dimethylformamide in which is dissolved hydrogen halide results in cis-reversion of the lactone ring and l-6β-hydroxy-3-oxoeu-santona-1, 4-dienic lactone (VIIIa), or l-santonin C is formed. In this reaction, a linear-conjugated dienone compound (IXa), formed by the shift of the double bond, and l-α-desmotroposantonin (Va) are produced as by-products, as well as a compound assumed to be the trienone (Xa), with an increase of one double bond. These new rearrangement reactions also proceed similarly in racemic compounds and rac-santonin C (VIIIb) is formed from rac-α-santonin (Ib), and rac-santonin D (XII) from rac-β-santonin (XI).抄録全体を表示PDF形式でダウンロード (730K) -
サントニンの新転位反応II α-サントニン合成中間体への応用石川 尚1956 年 76 巻 5 号 p. 507-510
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーTreatment of several intermediates of santonin synthesis, possessing the trans-lactone ring, with dimethylformamide containing hydrogen halide results in isomerization of the lactone ring to cis-form and the corresponding isomers are formed. This rearrangement reaction was utilized in clarifying the steric configuration of the two kinds of monoesters (XX and XXIV), obtained by partial saponification of ethyl 11-ethoxycarbonyl-3-oxoeusanton-4-enate (XI), and the cis-lactonic esters derived from them.抄録全体を表示PDF形式でダウンロード (671K) -
ラット肝切片による代謝高畠 英伍1956 年 76 巻 5 号 p. 511-514
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーThe in vitro metabolism of ethylhexabital (EHB) was examined by incubating a rat liver slice with ethylhexabital in a Krebs-Ringer phosphate buffer containing 0.2% glucose, and the formation of 3-keto-EHB (5-(3′-oxo-1′-cyclohexen-1′-yl)-5-ethylbarbituric acid), a metabolite in the case of in vivo metabolism, was identified by paper chromatography, and the amount formed and the amount of unchanged EHB remaining were determined at the same time by ultraviolet spectrophotometry. The amount of 3-keto-EHB formed reaches the maximum by incubation in pH 7.4 at 38° for 3 hours, with 750γ EHB for 500mg. of the liver slices. The action of liver brei is much weaker than its slice, while the action of the liver homogenate, kidney slice, and brain brei was much weaker but clearly indicated the formation of 3-keto-EHB. Pretreatment at 100° for 10 minutes or at 60° for 1 hour, or the addition of 0.02M potassium cyanide effect entirely no formation of 3-keto-EHB.抄録全体を表示PDF形式でダウンロード (579K) -
温度効果 その1松村 久吉, 井口 定男, 西田 守衞, 宮本 滋, 山本 孫兵衞, 岡室 トシ1956 年 76 巻 5 号 p. 515-520
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーIn order to examine the physicochemical stability of drugs, utilizing solubilization with nonionic surface active agents, a model experiment was carried out. Tween 80 was selected as the nonionic surfactant, used in a 10% aqueous solution, and caproic acid was used as the solubilizate. Test solutions were prepared with caproic acid solubilized with various amounts of 10% Tween 80 solution, and its physicochemical properties, such as surface tension, relative viscosity, density, lowering of freezing point, and pH, were continuously measured, in order to examine the effect of the micelle so formed by temperature changes and changes in the dispersion in the solution after preservation for a long period. Surfactant solution, especially with a solubilizate, shows sensitive and marked changes by warming or heating but when the solubilizate is a stable substance like caproic acid, the solution returns to the original state and the physicochemical properties also return to the normal, if the conditions are removed in short-time loading. In the case of preservations over a long period of time, the test solutions were found to undergo change which was incapable of returning to the original state.抄録全体を表示PDF形式でダウンロード (919K) -
N-(p-Acetamido及びp-Aminobenzenesulfonyl)-α-acetylpropionamidineの合成桶田 秀雄, 谷口 幹二, 榎 吉二, 山田 幸元, 荒木 正男1956 年 76 巻 5 号 p. 521-524
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーα-Acetylpropionic imidoether (I) and N4-acetylsulfanilamide (IIa) or sulfanilamide (IIb) undergo selective dealcoholation-condensation at N1-position of (II), in the presence of a basic substance, and form N-(p-acetamido- or p-aminobenzenesulfonyl)-α-acetylpropionamidine (IIIa or IIIb). In this reaction, basic reagent is required as a condensation agent and the solvent may be water, aliphatic alcohols or ketones, or pyridine, but the condensation does not occur in carbon tetrachloride, benzene, toluene, or ethyl acetate. When the condensation is carried out in a mixed solvent of the one (A) in which the condensation proceeds and the other (B) in which the condensation does not occur, the yield of the condensate differs with the mixing ratio of the solvents and the amount of condensation agent, the yield being good when (A) alone is used and decreases markedly as the amount of (B) increases. Hydrolysis of (III) with acid or alkali affords N-(p-acetamido- or p-aminobenzenesulfonyl) -α-acetylpropionamide (IVa or IVb) and (II) under mild conditions and (II) alone under drastic conditions. (III) forms its semicarbazone (Va or Vb) with semicarbazide hydrochloride and 5-(p-acet-amido- or -amino-benzenesulfonylamido)-3, 4-dimethylpyrazole (VIa or VIb) with hydrazine sulfate.抄録全体を表示PDF形式でダウンロード (580K) -
5-(p-Acetamido- 又はp-Amino-benzenesulfonylamido)-3,4-dimethylisoxazoleの合成桶田 秀雄, 谷口 幹二, 榎 吉二, 山田 幸元, 加納 三郎, 荒木 正男1956 年 76 巻 5 号 p. 525-527
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーApplication of hydroxylamine salt to N-(p-acetamido- or p-aminobenzenesulfonyl) α-acetylpropionamidine (I) affords 5-(p-acetamido- or p-aminobenzenesulfonylamido)-3, 4-dimethylisoxazole (II). The addition of a neutralization agent, such as potassium or sodium acetate, in this reaction affords, besides (II), an oxime (III) of (I) as an intermediate. Treatment of (III) with an equimolar amount of hydrochloric or acetic acid changes it quantitatively to (II), whose ultraviolet absorption maxima lie at 265mμ (IIa) and 274-275 mμ (IIb), agreeing with the values of the compounds synthesized by another route. Addition of a metal, such as zinc or iron, to the reaction of (I) and hydroxylamine salt results in a poor yield of (II), and (III) is obtained. The yield of (II) is also poor when iron is present in treating (III) with acid to form (II), and (III) is recovered.抄録全体を表示PDF形式でダウンロード (542K) -
Indan-1-one環の開環反応堀井 善一, 田村 恭光, 田中 邦彦, 掛見 英夫1956 年 76 巻 5 号 p. 527-530
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーIn an attempt to synthesize terracinoic acid, an alkaline degradation product of Terramycin, ring cleavage reaction of indan-1-one derivatives was examined as a synthetic method for the intermediate compound. Two kinds of processes were found by the utilization of the method of Johnson et al., the one (A-method) being derivation from 3-methylindan-1-one derivatives through the 2-bromo and 2-cyano compounds, and the other (B-method) through 2-hydroxymethylene and its bisoxime compounds, with subsequent hydrolysis to β-(2-carboxyphenyl) butyric acid derivatives in a good yield. It was also found that the oxidative cleavage of indan-1-one derivatives with sodium hypobromite afforded α-(2-carboxyphenyl)-acetic and propionic acid derivatives.抄録全体を表示PDF形式でダウンロード (866K) -
落合 英二, 森下 頴策1956 年 76 巻 5 号 p. 531-534
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーReaction of 4, 6-diaminoquinoline with 1 mole of acetic anhydride, acetyl chloride, or benzoyl chloride in pyridine chiefly affords a diacylated compound and recovery of the starting material, with a small amount of 6-benzoylamino derivative together with the recovery of the starting material and a dibenzoyl compound in the case of benzoylation. By heating 4, 6-diaminoquinoline with cyanuric acid chloride in acetone, in the presence of sodium carbonate, and heating the product with ethanolic ammonia or by reacting with 2-amino-4, 6-dichloro-s-trizine, bis (4-aminoquinolyl-6) melamine was obtained. Coupling of the diazotized 4, 6-diaminoquinoline with β-naphthol, 2, 6-diaminopyridine, 3-hydroxypyridine, or 8-hydroxypyridine afforded the corresponding 6-azo dyes. Antibacterial tests of these azo dyes and the melamine compound showed that none of them showed any better action than chloramphenicol and none possessed efficacy against Trypanosoma curzi. However, bis (4-aminoquinolyl-6) melamine and 4-amino-6-(2′, 6′-diaminopyridyl-3′) azoquinoline showed marked therapeutic effect against Trypanosoma gambiense.抄録全体を表示PDF形式でダウンロード (668K) -
ハナウド属のフロクマリンの分布藤田 路一, 古谷 力1956 年 76 巻 5 号 p. 535-537
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーThe ether extract of the root of Heracleum lanatum Michaux var. nipponicum (Kitag.) Hara, during the flowering season, yielded pimpinellin, isopimpinellin, isobergapten, and sphondin by the method shown in Table I. Further, bergapten and umbelliferone were isolated by paper chromatography. However, such furocoumarins were not detected in the leaves. Mature fruit yielded 3 kinds excluding isobergapten and sphondin, and umbelliferone (Table IV). In the present series of experiments, sphondylin, said to be one of the components of H. Sphondylium, was not detected. The ultraviolet spectra (Fig. 1) of these furocoumarins exhibited the maxima at around 250 mμ and 308 mμ.抄録全体を表示PDF形式でダウンロード (414K) -
シシウド属の一新クマリン成分について藤田 路一, 古谷 力1956 年 76 巻 5 号 p. 538-542
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーA kind of coumarin derivative was isolated from the ether extract of the root of Angelica schishiudo Koidz. This substance comes as white needle crystals of mp 130°, C16H16O5, and forms acetone and acetyl-5, 7-dimethoxycoumarin, C13H12O5, with 30% potassium hydroxide, phloroglucinol by alkali fusion, and 5, 7-dimethoxycoumarin with conc, sulfuric acid. The dihydro compounds affords 5, 7-dimethoxycoumarin and isovalerianic acid with conc. sulfuric acid. This substance and the alkaline degradation products give negative Emerson and Gibbs reactions, that it is assumed to possess the side chain in the 6-position. From these evidences, this was assumed to be a new substance, was named angelicone, and a structure of 5, 7-dimethoxy-6-(3, 3-dimethylacryloyl) coumarin (I) is proposed for it. Further, distribution of angelicone in the allied plants was examined by paper chromatography and the results are given in Table II.抄録全体を表示PDF形式でダウンロード (790K) -
シオール型Thiamine誘導体について その6 Thiamine燐酸エステル類のS-アセチル化とそのTransacetylation川崎 弌1956 年 76 巻 5 号 p. 543-545
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーThiamine monophosphate or diphosphate was acetylated with acetic anhydride in alkaline solution and passed through a column of ion exchanger, H-type Amberlite XE-64. By these means, S-acetylthiamine phosphates were obtained as practically pure crystals and their reaction with glutathione effected transacetylation to form S-acetylglutathione.抄録全体を表示PDF形式でダウンロード (488K) -
Kainic Acidおよびその異性体のオゾン酸化成績体に関する研究 (6) Methyl ketone体のMonoester体およびその還元成績体中守 律夫1956 年 76 巻 5 号 p. 545-550
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーAs reported previously, the lactonic compounds of α-kainic acid series were found to be the δ-lactone between C3 and C4 of the pyrrolidine ring and a similar assumptions were made for the structure of the lactonic compounds of α-allo-kainic acid series. Confirmation of this assumption was made in the present series of experiments.
Partial esterification of α-allomethyl ketone compound (α-allo-III) gives the α-allo-C3-monomethyl ester (α-allo-VII). In the same manner, β-allomethyl ketone compound (β-allo-III) yields β-allo-C3-monomethyl ester (β-allo-VII). On the other hand, the same reaction course in α- and β-series results in isomerization to form the corresponding α-allo and β-allo series monoester compounds. Partial hydrolysis of the diester of (α-allo-III) gives C2-monomethyl ester compound (α-allo-IX). By comparing the reduction products of (α-allo-VII) and (α-allo-IX), it was confirmed that the lactonic compounds of α-allokainic acid series were also δ-lactones formed between C3 and C4.抄録全体を表示PDF形式でダウンロード (869K) -
各地産のトリカブト植物塩基 その7 所謂ヤマトリカブトの塩基成分落合 英二, 岡本 敏彦, 坂井 進一郎, 金子 雅英, 藤沢 圭吾, 永井 右近, 谷 英郎1956 年 76 巻 5 号 p. 550-553
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーSome bases were isolated from two kinds of the so-called Aconitum japonicum Thunb. from different locale and the plants were found to possess entirely different componental bases. The species (Ochiai No. 6) from Nobeyama, Shin-shu, gives aconitine, mesaconitine, and a small amount of ignavine, while that (Ochiai No. 21) from Kogezawa, Mt. Takawo, does not afford these bases but Takawo base I (m.p. 196-198°, [α]D25: +72.6 (CHCl3), C23H27O7N3) and Takawo Base II (m.p. 260-261° (decomp.), [α]D28: +119.3° (MeOH)), together with isohypognavine and Shimoburo base II. Hydrolysis of isohypognavinol afforded, besides benzoic acid, a substance of m.p. 296°, [α]D15: +76.6° (MeOH), C20H27O4N, which gives a methiodide of m.p. 312° (decomp.), C20H25O3N⋅CH3I. This alkamine was named anhydroisohypognavinol.抄録全体を表示PDF形式でダウンロード (749K) -
酸化銅のみ充填せる装置におけるブランクの主要因について その1水上 聰, 宮原 景吉, 森田 ノブ1956 年 76 巻 5 号 p. 553-559
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーThe gas used for the carbon and hydrogen analyses is generally purified by heating to reduce the blank values, which should be as small as possible to increase accuracy. Such blank values were determined with three kinds of absorption tubes using the combustion tube described previously, and the large blank values were found to originate mostly in the connecting rubber tubes (including the wiping of absorption tubes). The use of an absorption tube with a metal needle (Mitsui's method) was found to give almost zero blank value, as long as considerations are given to the correction of dispersion.抄録全体を表示PDF形式でダウンロード (808K) -
酸化銅のみ充填せる装置におけるブランクの主要因について その2水上 聰, 宮原 景吉, 森田 ノブ1956 年 76 巻 5 号 p. 559-561
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーFurther examinations were made for eliminating the large blank values in carbon and hydrogen determination and majority of such values was found to be due to the connecting rubber tubes by cancelling the items on wiping of the absorption tube, which should be avoided as much as possible. The varied stop point of the balance was found to differ during non-loading period and during the determination.抄録全体を表示PDF形式でダウンロード (348K) -
Diphenyl Disulfide及びDiphenyl Sulfide誘導体より2-Chlorophenothiazineの合成 その1恩田 政行, 川西 正純, 大西 定夫, 富永 武, 功刀 吉晁, 笹本 光雄, 鈴木 真言1956 年 76 巻 5 号 p. 562-564
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーSynthesis of 2-chlorophenothiazine from diphenyl sulfides and disulfides was examined. Disulfides react with aniline in aniline solvent alone and sulfides in pyridine hydrochloride alone to form 2-chlorophenothiazine. Reduction of bis (2-nitro-4-chlorophenyl) disulfide with hydrazine causes partial desulf urization and 4, 4′-dichloro-2-amino-2′-nitrodiphenyl sulfide is formed as a by-product.抄録全体を表示PDF形式でダウンロード (537K) -
Diphenyl Sulfide誘導体より2-Chlorophenothiazineの合成 その2恩田 政行, 川西 正純, 大西 定夫, 富永 武, 功刀 吉晁, 笹本 光雄, 鈴木 真言1956 年 76 巻 5 号 p. 564-566
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーSynthesis of 2-chiorophenothiazine by the cyclization of diphenyl sulfides at 2 and 2′ positions was examined. Examples of such cyclization are rare but 4-chloro-2-acetamina-2′-bromodiphenyl sulfide easily undergoes cyclization to form a phenothiazine ring. Cyclization of 2, 2′-diamino-4-chlorodiphenyl sulfide by deammoniation is extremely difficult and the reaction proceeds only in aniline solvent, in the presence of aniline hydrochloride, although the cyclization does not occur between 2 and 2′ and is assumed to belong to the group of reactions described in the previous report.抄録全体を表示PDF形式でダウンロード (516K) -
Smiles転位によるPhenothiazine合成恩田 政行, 川西 正純, 大西 定夫, 富永 武, 功刀 吉晁, 笹本 光雄, 鈴木 真言1956 年 76 巻 5 号 p. 566-567
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーPreparation of phenothiazines from diphenyl sulfides by the Smiles rearrangement was examined. Heating of 4-chloro-2-acetamido-2′-nitro- and 4-chloro-2-nitro-2′-acetamidodiphenyl sulfide in quinoline effects deacetylation together with rearrangement and cyclization to form 2- and 3-chlorophenothiazines. 4, 4′-Dichloro-2-acetamido-2′-nitrodiphenyl sulfide affords 3, 7-dichlorophenothiazine by the usual method, in the presence of alkali hydroxide.抄録全体を表示PDF形式でダウンロード (314K) -
アンチピリン誘導体について その2高橋 酉蔵, 堀 幹夫, 兼松 顕1956 年 76 巻 5 号 p. 568-570
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリー4-Antipyrylurea (XII) was obtained in a good yield by reacting 4-aminoantipyrine (IV) and potassium cyanate in dilute acetic acid. Condensation of α-haloacyl halides and 4-methylaminoantipyrine (V), 4-amino-1, 2-diphenyl-3-methylpyrazol-5-one (XXII), and 4-antipyrylurea (XII) respectively afforded the 4-α-haloacylmethyl-aminoantipyrines (VI to VIII), 4-α -haloacylamino-1, 2-diphenyl-3-methylpyrazol 5-one (XXIII to XXIV), and 1-α-haloacyl-3-(4-antipyryl) ureas (XIII to XVI). These haloacyl derivatives were reacted with dimethyl- or diethylamine to prepare 4-α-dimethyl (or diethyl) aminoacylmethylaminoantipyrines (IX to XI), 4-α-dimethylaminoacylamino-1, 2-diphenyl-3-methylpyrazol-5-ones (XXV to XXVI), and 1-α-dimethyl (or diethyl) aminoacyl-3-(4-antipyryl) ureas (XVII to XXI).抄録全体を表示PDF形式でダウンロード (482K) -
抽出単離及びその構成糖について秋谷 七郎, 友田 正司1956 年 76 巻 5 号 p. 571-574
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーThe polysaccharide fraction extracted from a human placenta was acetylated and the acetate so obtained was fractionated by silica gel chromatography. The sugars were thereby isolated and componental sugars were examined.抄録全体を表示PDF形式でダウンロード (635K) -
グルコースより成る六糖体の構造秋谷 七郎, 友田 正司1956 年 76 巻 5 号 p. 575-577
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーThe structure of a glucan obtained from human placenta was examined and it was found to be a substance with a straight chain of six molecules of D-glucopyranose in C1-C4 bonding, with a reducing group at one end.抄録全体を表示PDF形式でダウンロード (383K) -
4-Methylcoumarin, Coumarin-3-carboxylic Acid Diethylamide及びBarbitalの催眠効力比及び安全指数について北川 晴雄1956 年 76 巻 5 号 p. 578-581
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリー4-Methylcoumarin, which has been found by past studies to possess comparatively good hypnotic activity and which shows hypnotic state symptomatically the same as that of barbital when administered to mice, and coumarin-3-carboxylic acid diethylamide, which shows hypnotic state different from that of barbital, were chosen to make a comparative examination of the hypnotic efficacy of these two derivatives and of barbital by the six-point assay method of parallel line assay. The result obtained was barbital=l>coumarin-3-carboxylic acid diethylamide=0.5767>4-methylcoumarin=0.52545. The safety index used to show the safety of pharmaceutics to date included (1) LD50/ED50 or ED50/LD50 and (2) SSM=(LD1/ED99-l)×100, the standard safety margin proposed by Foster. However, (1) gives no considerations for the distribution of ED and LD, while that is taken care of in (2) but extreme values such as LD1 and ED99 are estimated and goes contrary to the adoption of ED50 and LD50 proposed because the estimation of the values of LD1 and ED99 is too difficult. It is, therefore, proposed that a new safety index (Is) be adopted which would be represented by Is=1/σED (logLD5-logED50)=bED (XLD50-XED50), in which ED50 is taken for the effective dosis, bED as its distribution, and the more easily estimable LD5 as the lethal dose.
The safety indices for the foregoing three compounds were calculated and their safety was comparatively examined.抄録全体を表示PDF形式でダウンロード (684K) -
物理化学的性質及び生体内分布と催眠作用との関係について北川 晴雄1956 年 76 巻 5 号 p. 582-587
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーIn order to elucidate the mechanism of hypnotic action of coumarin derivatives, some physicochemical properties, more specifically its distribution ratio between ether and water and solubility in water, were measured and its adaptability to the theory of Meyer-Overton was examined. It was thereby found that the compounds possessing hypnotic action in mice generally possess large distribution ratio and those having no such action possessed small ratio, but there were many cases of exceptions. Studies on the in vivo distribution of hypnotics, especially in the brain and the liver, are important in connection with the theory of hypnosis and detoxication but actual research in this field is still small. Therefore, the in vivo distribution of 4-methylcoumarin, which possesses hypnotic acition, and 4-methylumbelliferone, which does not, were examined, especially in the brain and the liver by the Beckman spectrophotometer. As a result, it was found that these drugs were distributed in comparatively large amount in various tissues and that significant differences were not found, with 5% significance level, between the distribution into the brain and the liver of 4-methylcoumarin and 4-methylumbelliferone.抄録全体を表示PDF形式でダウンロード (1003K) -
呼吸酵素系に及ぼす影響について北川 晴雄1956 年 76 巻 5 号 p. 588-594
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーIt has previously been reported that the effect of coumarin derivatives on the tissue respiration of albino rat brain confirmed the theory of Quastel and his school. Which enzymatic system is affected in the chief course of biological oxidation of coumarin derivatives was examined to see whether this was due to the suppressive action on the cytochrome level, as in hypnotic-anesthetics in general, as proposed by Michaelis and Quastel, or by the suppressive action on the dehydrogenase level, such as in steroids, as proposed by Gordan et al.. It was thereby concluded that the coumarin derivatives showed suppressive action against the cytochrome-cytochrome oxidase system as in hypnotic-anesthetics in general, and that their action mechanism was fundamentally different from the hypnotic action of steroids.抄録全体を表示PDF形式でダウンロード (1143K) -
C-17位に水酸基を有するステロイドの呈色反応に就いて (補遺)和田 俊洋1956 年 76 巻 5 号 p. 595-596
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーCortisone and 17α-hydroxyprogesterone possess a tertiary hydroxyl in 17α-position and would seem liable to undergo coloration by warming with an acid but the color actually does not appear. The reason for it is the presence of a carbonyl at C20 and its reduction makes it easier to color with an acid.抄録全体を表示PDF形式でダウンロード (330K) -
メギのアルカロイド研究 その2富田 眞雄, 菊池 徹1956 年 76 巻 5 号 p. 597-599
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーFrom a mixture of quaternary bases contained in Berberis Thunbergii DC., berberine-type base was removed as the iodide, and two kinds of bases were further obtained from the mother liquor as picrates; orange microprisms (A), m. p. 217-220° (decomp.), and bright yellow microprisms (B), m. p. 224-225° (decomp.). It was found that the picrate (A) is jatrorrhizine picrate and picrate (B), magnoflorine picrate.抄録全体を表示PDF形式でダウンロード (528K) -
ヒイラギナンテンのアルカロイド その4富田 眞雄, 久郷 威彦1956 年 76 巻 5 号 p. 599-600
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーMagnoflorine, a quaternary base of the aporphine type, was also detected in Mahonia japonica DC., as in the Berberis genus such as Perberis Thunbergii DC. and B. amurensis Rupr. var. japonica (Regel) Rehd. forma Bretschneideri (Rehd.) Ohwi.抄録全体を表示PDF形式でダウンロード (350K) -
酸化銅及び酸化銅, 銀のみ充填せる装置について水上 聰, 家城 忠義, 森田 ノブ1956 年 76 巻 5 号 p. 601-604
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーThe largest cause of error in the carbon and hydrogen analysis is the presence of lead peroxide in the apparatus and lead peroxide is not required in the elementary analysis of compounds composed of carbon, hydrogen, and oxygen. Experiments were conducted by filling the combustion tube with copper oxide alone and the determination of blank values was carried out, examining the effect of atmospheric moisture and carbon dioxide. It was found that this method gave satisfactory results, even in steroidal compounds where the content of carbon is large. Satisfactory results were also obtained by filling the tip of the combustion tube with rolls of silver wire and submitting compounds composed of carbon, hydrogen, oxygen, halogen, and sulfur to analyses.抄録全体を表示PDF形式でダウンロード (425K) -
Piperazine及びTrimethylethylenediamine誘導体の合成藤井 輝一, 重松 暹1956 年 76 巻 5 号 p. 605-607
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーAn antifilarial, 1-diethylcarbamoyl-4-methylpiperazine, was obtained by the reaction of diethylamine, either directly or in the presence of alkali hydroxide, with 1-methyl-4-piperazinecarboxylic chloride, obtained by the reaction of phosgene and N-methylpiperazine. A few derivatives of N-methylpiperazine were also prepared. The corresponding derivatives of N, N′-dimethylethylenediamine, formed by the C-C cleavage of N-methylpiperazine, were obtained.抄録全体を表示PDF形式でダウンロード (622K) -
Formylpiperazineによるホルミル化藤井 輝一, 湯川 敦彦1956 年 76 巻 5 号 p. 607-608
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーBy the reaction of dialkylaniline and thiophene with 1-formyl- or 1, 4-diformylpiperazine and phosphoryl chloride, the corresponding aldehydes, i.e. 2-thienaldehyde and p-dialkylaminobenzaldehyde, were obtained. The yield of the product was 59-77% when 1, 4-diformylpiperazine was used and 48-55% when 1-fomyl derivative was used, showing the yield to be better in all cases when 1, 4-diformyl derivative was used.抄録全体を表示PDF形式でダウンロード (333K) -
秋谷 七郎, 中沢 泰男, 石倉 俊治1956 年 76 巻 5 号 p. 608-610
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーCodeine can be colorimetrically determined by its oxidation with potassium permanganate in hydrochloric acidity, colored by the addition of sodium chromotropate, and sulfuric acid, and spectrometric determination made at 580mμ. This color is caused by formaldehyde formed by the oxidative decomposition of the methoxyl and N-methyl groups in codeine.抄録全体を表示PDF形式でダウンロード (990K) -
刈米 達夫, 高橋 三雄, 新田 あや, 常久 芳直1956 年 76 巻 5 号 p. 611
発行日: 1956/05/25
公開日: 2010/02/19
ジャーナル フリーPDF形式でダウンロード (137K)
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