巻号一覧
86 巻, 7 号
選択された号の論文の18件中1～18を表示しています
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藤沢 正計, 河村 光雄1966 年 86 巻 7 号 p. 541-543
発行日: 1966/07/25
公開日: 2008/05/30
ジャーナル フリーIn order to confirm the photodecomposition products of phenothiazine drugs, 2-chloro-phenothiazin-7-one (II) and 7-oxo-2-phenothiazinecarbonitrile (III), N, N-dimethyl-7-oxo-2-phenothiazinesulfonamide (IV), and 2-methoxyphenothiazin-3-one (V) were synthesized as the standard samples by the method of Pummerer and Gassner. Position of the oxidized site in phenothiazine ring was assumed from comparison of NMR and IR spectra of these synthesized compounds with those of phenothiazin-3-one (I).抄録全体を表示PDF形式でダウンロード (442K) -
岡野 定輔, 合屋 周次郎, 津田 宣直1966 年 86 巻 7 号 p. 544-547
発行日: 1966/07/25
公開日: 2008/05/30
ジャーナル フリーA new method for the synthesis of 3-aminoisoquinoline derivatives was described, where methyl ο-cyanomethylbenzoate was treated with aqueous amines under mild conditions to yield isoquinoline ring with amino group in 3-position. The mode of reaction was also proposed. Amination of 1, 3-dichloroisoquinoline gave 1-amino-3-chloroisoquinoline alone.抄録全体を表示PDF形式でダウンロード (533K) -
岡野 定輔, 児島 昭次1966 年 86 巻 7 号 p. 547-554
発行日: 1966/07/25
公開日: 2008/05/30
ジャーナル フリーHalf-neutralization potentials (HNP) of non-aqueous titration of 22 pyrimidine derivatives and 10 purine derivatives have been set against pKa (H2O) values determined by spectrophotometry. Linear relationship exists between HNP and pKa of most of the pyrimidine and purine derivatives (Figs. 3 and 4), and pKa values calculated with the algebraic expression of these relations (formulas 1-7), using the observed non-aqueous HNP values, correspond with the spectrophotometric pKa data with the error limit of ±0.5 (Tables I-V). Methylcellosolve-acetonitrile mixture shows greater resolving power than acetic acid-acetic anhydride mixture as non-aqueous solvent for the potentiometric titration of pyrimidine and purine derivatives with perchloric acid.抄録全体を表示PDF形式でダウンロード (876K) -
田中 信夫, 松下 博一, 内海 勇1966 年 86 巻 7 号 p. 554-557
発行日: 1966/07/25
公開日: 2008/05/30
ジャーナル フリーAlthough tablets of calcium p-aminosalicylate undergo rapid disintegration immediately after tabletting, the time of disintegration is prolonged with passage of time. This phenomenon was assumed to be due to the gradual formation of a hexahydrate from the anhydrate by the presence of a slight amount of free water in the tablets. It was found that there was no quantitative correlation between the water content in the powder or granules for tabletting of calcium p-aminosalicylate and the amount of amorphous substance contained in its anhydrate, so that the quantitative determination of an anhydrate cannot be defined from the water content alone. It was found through utilization of heat generation from this amorphous substance of the anhydrate when soaked in water that there is a correlation between the quantity of heat generated and amount of the amorphous substance. Therefore, a high-sensitivity calorimeter, whose sensitivity for temperature detection was in the order of ±5°×10-5, was devised and quantitative determination of amorphous substance in the tablets or granules was carried out. Examination of a relationship between the quantity of heat generated and time of disintegration of tablets gave results listed in Table II.抄録全体を表示PDF形式でダウンロード (538K) -
浜元 要, 堀木 樟夫, 池上 昭子, 武田 健一1966 年 86 巻 7 号 p. 558-564
発行日: 1966/07/25
公開日: 2008/05/30
ジャーナル フリーFollowing the previous work, synthesis of steroidal hormone intermediates was attempted from metagenin (Ia) and nogiragenin (XIa), and one of the most important compound, 25D-spirosta-1, 4, 9(11)-trien-3-one (Va), was obtained by bromination of 2, 11-dimesyloxy-3-one (IIb) and Δ9(11)-2-tosyloxy-3-one (VIIIa) derived from metagenin (Ia) followed by dehydro-bromination. Other related derivatives were also prepared.抄録全体を表示PDF形式でダウンロード (866K) -
浜元 要, 堀木 樟夫, 前園 憲英1966 年 86 巻 7 号 p. 565-570
発行日: 1966/07/25
公開日: 2008/05/30
ジャーナル フリーSynthesis of 17α-hydroxy-5β-pregna-1, 9(11)-diene-3, 20-dione and pregna-1, 4, 9(11)-triene-3, 20-dione from 2β, 3β, 11α-trihydroxy-5β-pregn-16-en-20-one triacetate, derived from metagenin (5β, 25D-spirostane-2β, 3β, 11α-triol), is described. Tosylation of 2β, 3β, 17α-trihydroxy-5β-pregn-9(11)-en-20-one and 2β, 3β-dihydroxy-5β-pregn-9(11)-en-20-one gave a mixture of 2-monotosylate and 2, 3-ditosylate. The amount of ditosylate formed was found to be greater than in the case of spirostane series previously reported.抄録全体を表示PDF形式でダウンロード (748K) -
林 英作, 飯島 千穂子1966 年 86 巻 7 号 p. 571-576
発行日: 1966/07/25
公開日: 2008/05/30
ジャーナル フリーIn continuation of the previous work, 1) examinations were made on the reaction between 2-phenylquinoxaline 4-oxide (I) and phenylmagnesium bromide. 1) Heating of I and phenylmagnesium bromide in a mixed solvent of ether and benzene, followed by hydrolysis, and varying the time of heating from 1 to 9 hours, failed to show any distinct relationship between heating time and the ratio of the products, 2, 3-dithenylquinoxaline (II) and 2, 3-diphenylquinoxaline 1-oxide (III) (Table I). 2) Addition of p-benzoquinone prior to hydrolysis after heating and refluxing I and phenylmagnesium bromide as above, resulted in overwhelming formation of III over II with shortening of the heating period. Amount of III formed decreased with extension of the heating time and, with the same period of heating, addition of p-benzoquinone increased the amount of III formed (Table II). These experimental results indicate that the reaction process can be illustrated as shown in Chart 2, similar to that proposed by Kato and Yamanaka7, 8) (Chart 1). Reaction of I with alkylmagnesium halide as the Grignard compound gave results listed in Table III. In this case, when the alkyl was tert-butyl and benzyl, I underwent deoxidation to form 2-phenylquinoxaline (XV), with additional formation of 2-tert-butyl-3-phenyl-1, 2-dihydroquinoxaline (XVI) in the cast of tert-butyl. The reaction process in this case may probably be represented as shown in Chart 3.抄録全体を表示PDF形式でダウンロード (706K) -
林 英作, 大石 悦男1966 年 86 巻 7 号 p. 576-584
発行日: 1966/07/25
公開日: 2008/05/30
ジャーナル フリーApplication of monoperphthalic acid to 1-phenylphthalazine (I) affords only one kind of monoxide, 1-phenylphthalazine 3-oxide (II). Application of phosphoryl chloride or sulfuryl chloride to II produces the expected 1-chloro-4-phenylphthalazine (XV). Application of acetic anhydride to II failed to afford any product of known structure. Application of benzoyl chloride and potassium cyanide to II gave the expected 4-phenyl-1-phthalazinecarbonitrile (XVIII), while application of tosyl chloride to II in the presence of alkali gave the expected 4-phenyl-1(2H)-phthalazinone (XIV) and XV, but both in a poor yield. Reaction of II and phenyl isocyanate gave the expected 1-anilino-4-phenylphthalazine (XX), also in a poor yield. Application of the Grignard agent, phenyl- or isopropyl-magnesium bromide, to II gave 1, 4-diphenylphthalazine 2-oxide (X) or 1-isopropyl-4-phenylphthalazine 2-oxide (XII). In these reactions, the poor yield of the expected product was accompanied in majority of cases with viscous substance of unknown structure.抄録全体を表示PDF形式でダウンロード (1053K) -
岩佐 準三, 成戸 俊介1966 年 86 巻 7 号 p. 585-590
発行日: 1966/07/25
公開日: 2008/05/30
ジャーナル フリーHypaconitine (0.048%), aconitine (0.010%), and mesaconitine (0.006%) were isolated from Aconitum carmichaeli DEBX. (crude drug Sen-uzu) by means of alumina column chromatography. A new alkaloid, tentatively named carmichaeline, was isolated from the water-soluble basic fraction as colorless prisms, m.p. 185∼186°, C22H35O4N, [a]25D-16.7°.抄録全体を表示PDF形式でダウンロード (704K) -
松本 久男1966 年 86 巻 7 号 p. 590-599
発行日: 1966/07/25
公開日: 2008/05/30
ジャーナル フリーTheoretical equations of drug absorption from the intestine were derived assuming that permeability characteristic of the intestina1 membrane is not affected by Tween 80 solutions, and that the same mechanism as previously investigated employing a cellulose membrane is applicable. Results of recirculating absorption experiments through rat small intestine in vitro and in situ using benzocaine and sulfisoxazole, thought to be absorbed by passive diffusion, solubilized in the Tween solutions evidenced that these equations are well applicable and the membrane permeability remains unaffected. An equation was derived for the relationship between ratio, r' (total/free drug molecules), in the surfactant solutions and pH of the recirculating solutions, and its applicability was ascertained by means of solubility method and equilibrium dialysis method. In order to investigate kinetically the effect of nonionic surfactants on the rapidity of absorption of drugs at various pH, the latter equation was introduced into the former equations and their applicability was also ascertained using sulfisoxazole with the recirculation method in situ at pH 3.1, 4.9, and 7.4. Then, the other equation showing the relationship between amounts of administrated and absorbed drugs from the nonionic surfactant solutions was derived and it applied well to the results of absorption experiments on sulfisoxazole after 30 or 60 minutes' recirculation in situ. Therefore it became possible to anticipate the amount of drugs to be absorbed from the small intestinal tract containing Tween 80 solution.抄録全体を表示PDF形式でダウンロード (976K) -
板谷 元一, 高井 義治, 貝谷 トヨ1966 年 86 巻 7 号 p. 600-608
発行日: 1966/07/25
公開日: 2008/05/30
ジャーナル フリーTwo routes, A and B, shown in Chart 1 were experimentally examined for the syntheses of title compounds, 2-[p-(substitutedsulfamoyl)pheny1]benzimidazoles (XIX and XX). Method A was found to be unsuitable but method B was available for the synthesis of majority of these compounds. Use of ethylene glycol as a solvent was found to be suitable in this case. Compounds which could not be synthesized by method B or which were obtained only in a low yield were prepared by route C shown in Chart 2. By the use of these three methods, 28 kinds of derivatives listed in Table III, which are all new compounds, were synthesized. Ultraviolet Spectra (Fig. 2) of five (XIX-1, -2, -15, XX-1, -7) of these compounds indicated that their absorption maxima had shifted to a longer wave-length region and had become broad, as in the case of 2-phenylbenzimidazole9) and 2-styrylbenzimidazole.抄録全体を表示PDF形式でダウンロード (843K) -
永田 正典1966 年 86 巻 7 号 p. 608-613
発行日: 1966/07/25
公開日: 2008/05/30
ジャーナル フリーReaction of quinaldyllithium with bromoacetaldehyde acetal gave 2-quinolinepropionaldehyde acetal (VII) whose reduction over platinum oxide catalyst at a high pressure at room temperature yielded 1, 2, 3, 4-tetrahydroquinoline-2-propionaldehyde acetal (VIII). 1-Nitroso-1, 2, 3, 4-tetrahydroquinoline-2-propionaldehyde acetal (IX), obtained by nitrosation of VIII in acetic acid at 0°, was reduced by lithiumaluminum hydride to 1-amino compound (X), which was heated with oxalic acid in alcoholic solution, followed by cyclization to 4, 4a, 5, 6-tetrahydro-3H-pyricdazo[2, 3-α]quinoline (XI). Acetic acid solution of XI absorbed one mole of hydrogen over platinum oxide catalyst to give 2, 3, 4, 4a, 5, 6-hexahydro-1H-pyridazo[2, 3-α]quinoline (VI).抄録全体を表示PDF形式でダウンロード (760K) -
永田 正典1966 年 86 巻 7 号 p. 613-616
発行日: 1966/07/25
公開日: 2008/05/30
ジャーナル フリーEthyl 1-(ethoxycarbonylisopropylidene)amino-1, 2, 3, 4-tetrahydro-2-quinolinecarboxylate (IV), obtained by heating ethyl 1-amino-1, 2, 3, 4-tetrahydro-2-quinolinecarboxylate with ethyl aceto-acetate, was cyclized to the corresponding keto ester (V, Va, or Vb) at 110°, in the presence of sodium ethoxide. The difference between Va and Vb lies in the presence of an intra-molecular hydrogen bonding in Va and a free enol form of keto ester in Vb.抄録全体を表示PDF形式でダウンロード (538K) -
伊藤 真純, 杉原 明1966 年 86 巻 7 号 p. 617-622
発行日: 1966/07/25
公開日: 2008/05/30
ジャーナル フリーSome nitrofuran derivatives were synthesized as possible chemotherapeutic agents. 3-(5-Nitro-2-furyl)acryloyl chloride was condensed with diethyl malonate, ethyl tert-butyl malonate, ethyl acetoacetate, and 2-acetyl-γ-bytyrolactone to give diethyl 3-(5-nitro-2-furyl)-acryloyl malonate (IIa) and other related derivatives. IIa was hydrolyzed to ethyl 3-(5-nitro-2-furyl)acryloyl acetate (IIe), which was condensed with hydrazine and phenylhydrazine to give related 2-pyrazolin-5-one derivatives. Anti-microbial activity of these compounds are listed in the Table.抄録全体を表示PDF形式でダウンロード (650K) -
田上 昇一郎, 笹山 浩三郎, 志甫 伝逸1966 年 86 巻 7 号 p. 622-627
発行日: 1966/07/25
公開日: 2008/05/30
ジャーナル フリーPyrolysis of para-substituted benzaldehyde hydrazones yields a 1-substituted s-triazolo-[4, 3-α]quinoxaline with exclusive elimination of hydrogen. Kinetics of this pyrolysis reaction was examined and isokinetic relationship for this type of cleavage was presented. Possible explanations of these facts are discussed.抄録全体を表示PDF形式でダウンロード (553K) -
谷山 兵三, 北川 常広, 三浦 孝子1966 年 86 巻 7 号 p. 628-630
発行日: 1966/07/25
公開日: 2008/05/30
ジャーナル フリーA new synthetic method was attempted for the preparation of alkoxyphenylthiourea derivatives which are regarded of value as a chemotherapeutic for tuberculosis and leprosy. Refluxing of 2-thio-3-(p-alkoxyphenyl)-4-thiazolidinone6) and p-alkoxyphenylamines in an oil bath or heating of a mixture of these two compounds sealed in a tube resulted in the formation of objective thiourea derivatives with the same or different alkoxyphenyl groups in the para- and para'-positions. In this reaction, heating of the mixture in a sealed tube gave better yield with less formation of resinous by-product.抄録全体を表示PDF形式でダウンロード (391K) -
石井 永, 小牧 竜夫1966 年 86 巻 7 号 p. 631-633
発行日: 1966/07/25
公開日: 2008/05/30
ジャーナル フリーAlkaloidal components were examined with the root of Xanthoxylum ailanthoides SIEB. et ZUCC. (Fagara ailanthoides (SIEB. et ZUCC.) ENGL.) (Japanese name "Karasu-zansho"). The tertiary furoquinoline-type alkaloids, dictamnine (II), m.p. 133∼135.5°, and skimmianine (III), m.p. 176∼177°, the quaternary benzophenanthridine-type base, nitidine (V) chloride, m.p. 274∼275°, and a water-soluble quaternary aporphine-type base, laurifoline (I) chloride, m.p. 253°, were isolated. Presence of a neutral substance, xanthyletin (VI), m.p. 132∼133°, a dimethylpyranocoumarin, was alse revealed.抄録全体を表示PDF形式でダウンロード (497K) -
佐々木 喜男1966 年 86 巻 7 号 p. 634-636
発行日: 1966/07/25
公開日: 2008/05/30
ジャーナル フリーExaminations were made on the absorption maximum and absorbancy of the k-band exhibited by the chromophore group, α, β-unsaturated C=O in 2- and 6-substituted-Δ4-3-ketosteroids. These spectral characteristics were found to be due to changes in spatial configuration of the chromophore group accompanying changes in steric structure.抄録全体を表示PDF形式でダウンロード (353K)
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