巻号一覧
89 巻, 5 号
選択された号の論文の25件中1～25を表示しています
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別所 貞雄, 富岡 穂一, 伊藤 四郎1969 年 89 巻 5 号 p. 599-606
発行日: 1969/05/25
公開日: 2008/05/30
ジャーナル フリーIt is important to consider the pressure transmission in tablet compression designs. Pressure transmission in the two directions, the compression and the die wall direction, were measured for several substances, racked weimhts and compression pressures. The experimental equation in the compression direction is PL=kPU in pressure region 50-4000 kg/cm2, which is usually used in pharmaceutical tablet compression. The presumption equation for pressure transmission ratio, k, in the compression direction is k=exp (-μKCm/A2) theoretically. And the presumption equation for the pressure transmission in mixture and multi-layer compression is PL=k1·k2···.kn·PU. The theoretical pressure transmission equation in the die wall direction is PD=D/4μS·(1-exp (-4μKS/D)) PU, but the fitness is worse experimentally than in the compression direction.抄録全体を表示PDF形式でダウンロード (861K) -
乙益 寛隆, 大宮 茂1969 年 89 巻 5 号 p. 607-609
発行日: 1969/05/25
公開日: 2008/05/30
ジャーナル フリー11-Oxo-11H-indeno [1, 2-b] quinoxaline (I) was reduced catalytically with Pd-C to give the corresponding alcohol (II). By the reaction of I with NaOC2H5, the ring-cleavage occured and 2-(3-hydroxy-2-quinoxalinyl) benzoic acid (IV) was obtained. IV was also prepared by the condensation of o-phenylenediamine and phthalonic anhydride. Treatment of IV it H2SO4 or PCl5 gave the dehydrated intramolecular ester (V), which was readily returned to IV with dil. alkali solution. I reacted with PCl5 to give the 11, 11-dichloro derivative (VI) and with hydroxylamine to form its oxine (VII). VII was converted into 6-oxo-5, 6-dihydroisoquino [3, 4-b] quinoxaline (VIII) in good yield by Beckmann rearrangement using PCl5 in CHCl3, and VIII was identical with the condensation product of o-phenylenediamine and phthalonimide by Gabriel method.抄録全体を表示PDF形式でダウンロード (448K) -
亀谷 哲治, 菅原 勉, 福本 圭一郎1969 年 89 巻 5 号 p. 610-616
発行日: 1969/05/25
公開日: 2008/05/30
ジャーナル フリーThe Bischler-Napieralski reactiorx of N-(5-benzyloxy-3, 4-dimethoxyphenethyl)-2-(3-benzyloxy-4-methoxyphenyl) acetamide (VI) gave a mixture of 3, 4-dihydroisoquinolines cyclized in the ortho-and para-position of the 5-benzyloxy group. Without isolation, the mixture was derived to the 1, 2, 3, 4-tetrahydroisoquinoline compounds, and separated into 8-hydroxy (XI) and 6-hydroxy (XII) compounds. The mixture of XI and XII was submitted to the Mannich reaction and the product was methylated with diazomethane to 1, 2, 3, 10, 11-pentamethoxyprotoberberine (XIV). The Bischler-Napieralski reaction of N-(5-benzyloxy-3, 4-dimethoxyphenethyl)-3-(3-ethoxycarbonyl-4-methoxyphenyl) propionamide (XX) also gave a mixture of 3, 4-dihydroisoquinolines which was derived to the 1, 2, 3, 4-tetrahydroisoquinolines and separated into 8-hydroxy (XXIV) and 6-hydroxy (XXV) compounds. Discrimination of 8-and 6-hydroxyisoquinolines was made from infrared and nuclear magnetic resonance spectral data. An attempted synthesis of the so-called 'homocularine' by the phenolic oxidation of the former XXIV, 6, 7-dimethoxy-8-hydroxy-1-(4-hydroxy-3-methoxyphenethyl)-2-methyl-1, 2, 3, 4-tetrahydroisoquinoline, did not materialize.抄録全体を表示PDF形式でダウンロード (742K) -
赤 輝也, 渡辺 慶昭1969 年 89 巻 5 号 p. 617-626
発行日: 1969/05/25
公開日: 2008/05/30
ジャーナル フリーIn continuation of the previous work on analgesics, 10 kinds of 5-substituted 1-(2-diethylaminoethyl)-2-(p-ethoxyphenylthio) benzimidazole were synthesized and tested but none of them showed any marked effect. Some of the previously prepared 5-unsubstituted 1-(2-tert-aminoethyl)-2-(P-substituted phenylthio) benzimidazoles showed a powerful analgesic effect. Comparison of infrared and nuclear magnetic resonance spectra of these two series of compounds showed a distinct difference between them in the absorption considered to be due to CH2 neighboring the nitrogen in diethylaminoethyl group in 1-position, the former showing absorption at around 2800 cm-1 which is absent in the latter. The nuclear magnetic resonance signal of the latter is shifted to a lower magnetic field than that in the former. These evidences suggest a difference in the steric structure of the diethylaminoethyl group in 1-position of the two series of compounds and this difference may be related to their pharmacological effect.抄録全体を表示PDF形式でダウンロード (917K) -
大木 貞雄, 長瀬 祐之助, 吉野 元世, 東 禎子, 浜口 文子1969 年 89 巻 5 号 p. 627-632
発行日: 1969/05/25
公開日: 2008/05/30
ジャーナル フリーThe benzoyl compounds (VII and XI) were prepared from 1-ethyl-and 1, 2-dimethyl-3-pyrrolidinecarboxylic chloride (VI and X), and VI and X were reacted respectively with cyclohexyl-and cyclopentyl-magnesium chloride to form 1-ethyl-α-cyclohexyl-and 1-ethyl-α-cyclopentyl-α-phenyl-3-pyrrolidinemethanol (II and III), and 1, 2-dimethyl-α-cyclohexyl-α-phenyl-3-pyrrolidinemethanol (IV).抄録全体を表示PDF形式でダウンロード (576K) -
大木 貞雄, 東 禎子, 長瀬 祐之助1969 年 89 巻 5 号 p. 633-637
発行日: 1969/05/25
公開日: 2008/05/30
ジャーナル フリーIn order to examine pharmacological activities, 1, 2-dimethyl-3-[bis(2-thienyl) methylene] pyrrolidine (I) and 1-[1, 1-bis(2-thienyl)-3-propemyl]-2-methylpyrrolidine were synthesized. I and II are prepared by Grignard reaction between either ethyl 1, 2-dimethyl-3-pyrrolidinecarboxylate (IV) or ethyl 2-methyl-1-pyrrolidinepropionate (XI) and 2-thienylmagnesium bromide, followed by the dehydration. A special examination was made on the novel synthesis of IV from the starting material ethyl 2-cyanomethylacetoacetate.抄録全体を表示PDF形式でダウンロード (569K) -
亀谷 哲治, 八巻 一弥, 小笠原 国郎1969 年 89 巻 5 号 p. 638-640
発行日: 1969/05/25
公開日: 2008/05/30
ジャーナル フリーDiveratryl ether (III), which had been obtained by the Williamson's method or by catalytic hydrogenation, was found to be formed through hydride transfer reduction in case of crossed Cannizzaro reaction. Furthermore, treatment of III with sulfuric acid gave its trimer (VI).抄録全体を表示PDF形式でダウンロード (399K) -
浜名 政和, 野田 浩司1969 年 89 巻 5 号 p. 641-644
発行日: 1969/05/25
公開日: 2008/05/30
ジャーナル フリーThe reactions of quinoline-, isoquinoline-, pyridine-, lepidine-, 4-chloroquinoline and 4-chloropyridine 1-oxides with morpholine enamine of isobutyraldehyde in the presence of benzoyl- or tosyl-chloride were examined. Both of these reactions at room temperature and under refluxing, afforded 2-(α-heterocyclyl) isobutyraldehydes in rather good yields. The structures of the products were confirmed by the infrared and nuclear magnetic resonance spectra examinations.抄録全体を表示PDF形式でダウンロード (535K) -
飯田 英夫, 菊地 豊彦, 桜井 邦好, 渡辺 徳弘1969 年 89 巻 5 号 p. 645-648
発行日: 1969/05/25
公開日: 2008/05/30
ジャーナル フリーCondensation of 5-bromo-3, 4-dimethoxyphenethylamine (II) and methyl ο-benzyloxy-phenylacetate (III) gave the amide (IV). The Bischler-Napieralski reaction of IV gave 3, 4-dihydroisoquinoline compound (V), and reduction of its methiodide with sodium borohydride, followed by debenzylation gave the phenolic base (IX). Intramolecular Ullmann reaction of phenolic base (IX) in the presence of potassium carbonate and cupric oxide in pyridine finally gave the objective 10, 11-dimethoxy-6-methyl-5, 5a, 6, 7, 8-pentahydro [l] benzoxepino [7, 6, 5-i, j] isoquinoline (X) as pale yellow oil, which was characterized as its oxalate of mp 188-190°.抄録全体を表示PDF形式でダウンロード (465K) -
金子 秀彦, 長束 輝1969 年 89 巻 5 号 p. 649-659
発行日: 1969/05/25
公開日: 2008/05/30
ジャーナル フリーFrom the reaction of 1-aminoisoquinoline with C-ethylated diethyl malonate and/or monoethyl diethylmalonate chloride, 3, 4-dihydro-2, 4-dioxo-2H-pyrimido [2, 1-α] isoquinolines (IIa-c) were obtained which easily converted to the corresponding tetrahydro compounds (IXa-c) by catalytic hydrogenation, while treatment of ethyl α, α-diethyl-1, 2, 3, 4-tetrahydro-1-isoquinolineacetate with cyanic acid, isocyanate, or isothiocyanate afforded the corresponding carbamoyl compounds and thiocarbamoyl compounds (XIXa-f). Intramolecular cyclization of XIXa-f in the presence of sodium ethoxide resulted in formation of the desired products, hexahydro-2, 4-dioxo-2H-pyrimido [6, 1-α] isoquinolines (XXa-f).抄録全体を表示PDF形式でダウンロード (1102K) -
新田 義博, 池田 喜明, 白木 弥寿之1969 年 89 巻 5 号 p. 660-668
発行日: 1969/05/25
公開日: 2008/05/30
ジャーナル フリーIntroduction of 2-hydroxyethyl group into the nitrogen in 1-phenyl-2-aminoethanol derivative (III-1-3), and dl-and l-ephedrine hydrochlorides afforded dihydroxy compounds (IV-1-4 and VIII) which were chlorinated into a nitrogen mustard-type dichloro compounds (V-1-4 and IX), and the latter were reacted with primary amine (VI) to obtain 2-phenylpiperazine derivatives (VII-1-19 and X-1-2), (+)-1-(p-chlorobenzyl)-2-phenyl-3, 4-dimethylpiperazine (X-1) was prepared by the chlorination of l-ephedrine hydrochloride to L-(+)-threo-chloro compound (XI), its reaction with a primary amine to obtain(+)-diamino compound (XII), and treatment of XII with dibromoethane. The compounds so obtained were tested for increasing the coronary and peripheral (femoral artery) blood flow using dogs. Some nine of the compounds tested were found to increase coronary blood flow, more than three times that of aminophylline used as the control. Some considerations were also made on the relationship between chemical structure and pharmacological activity.抄録全体を表示PDF形式でダウンロード (925K) -
池田 喜明, 新田 義博, 山田 澄1969 年 89 巻 5 号 p. 669-676
発行日: 1969/05/25
公開日: 2008/05/30
ジャーナル フリーPiperazinoalkylbarbituric acid derivatives (VIII, IX, and X) were prepared by the introduction of phenobarbital and allobarbital into 1-and 1, 3-position of substituted piperazines with ethylene, propylene, and β-hydroxypropylene as the bonding bridge. These derivatives were obtained by the reaction of barbituric acid with unsymmetrically 1, 4-disubstituted piperazines having a functional group in the ω-position. Phenobarbital series compounds with ethylene as the bonding bridge were obtained by the reaction of 1-(2-bromoethyl)-5-ethyl-5-phenylbarbituric acid (VII) and monosubstituted piperazines. The compounds so obtained were tested for prolonged duration of hexobarbital sodium anesthesia, using mice, and general symptoms in mice was tested with two compounds by their intraperitoneal administration. Correlation between chemical structure and pharmacological activity was examined from these results.抄録全体を表示PDF形式でダウンロード (895K) -
池田 喜明1969 年 89 巻 5 号 p. 677-688
発行日: 1969/05/25
公開日: 2008/05/30
ジャーナル フリーIn order to examine their pharmacological activity on the circulatory system, some piperazinoalkyltheophylline derivatives (X, XI, XIV, XV) were synthesized. X, XI, and XIV were obtained by the reaction of 7-(ω-halogenoalkyl) theophyllines (VIII, IX) and 7-(2, 3-epoxypropyl) theophylline (XII) with monosubstituted piperazines (I), and also by the reaction of theophylline with unsymmetrically 1, 4-disubstituted piperazines (II, III, IV, V) with a functional group in ω-position. Application of 0.5 equivalent of VIII and XII to piperazine afforded 7-piperazinoalkyl-(and 2-hydroxypropyl)-theophyllines (XVI and XVII) which were reacted with halogenide (XXI) to form X and XIV. XVI and XVII were obtained by the hydrolysis of X and XIV having a carbonyl-containing substituent in the 4-position of piperazine, and subsequent application of hydrogen bromide. Reaction of piperazine with 2 equivalents each of VIII and XII afforded the corresponding bis compounds (XVIII and XIX).抄録全体を表示PDF形式でダウンロード (1159K) -
碓井 義郎1969 年 89 巻 5 号 p. 689-698
発行日: 1969/05/25
公開日: 2008/05/30
ジャーナル フリー3-Aminothiazoline-2-thiones, 4H-1, 3, 4-thiadiazine-2-thiols, and their derivatives were synthesized, and structure of their reaction intermediates was elucidated. It has been found that 3-arylideneamino-4-phenylthiazoline-2-thiones tend to decompose into aromatic nitriles and 4-phenylthiazole-2-thiol when heated to above their melting point. New synthetic method for nitriles from aldehydes that utilizes this thermal decomposition is described.抄録全体を表示PDF形式でダウンロード (955K) -
碓井 義郎, 山野 藤吾1969 年 89 巻 5 号 p. 699-701
発行日: 1969/05/25
公開日: 2008/05/30
ジャーナル フリーComparative examinations were made on the activities against several fungi using 3-aminothiazoline-2-thiones, 4H-1, 3, 4-thiadiazines, and their derivatives synthesized in earlier work, 1) and relationship between their structure and activity has been discussed.抄録全体を表示PDF形式でダウンロード (394K) -
清水 岑夫, 森田 直賢1969 年 89 巻 5 号 p. 702-704
発行日: 1969/05/25
公開日: 2008/05/30
ジャーナル フリーChrysosplenin, a flavonoid glicoside from C.japonicum (MAXIM.) MAKINO (japanese name "Yamanekonomeso"), had been assumed to be 3, 5, 4'-trihydroxy-6, 7, 3'-trimethoxyflavone monoglucoside.3) Using paper partition chromatography, however, chrysosplenin was revealed to be a mixture of I and II. I, mp 226-228°, C25H28O13·2H2O, was identified as chrysospenoside B4) and II, mp 163-165°, C24H26O13, was determined to be 5, 3', 4'-trihydroxy-6, 7, 3-trimethoxyflavone 4'-monoglucoside. We proposed the names chrysosplenoside D and chrysospenol D for the glycoside and its aglycone, respectively.抄録全体を表示PDF形式でダウンロード (478K) -
有澤 宗久, 中沖 太七郎1969 年 89 巻 5 号 p. 705-706
発行日: 1969/05/25
公開日: 2008/05/30
ジャーナル フリーThe fresh lieves of Sorbaria stellipila SCHNEID. (=Sorbaria sorbifolia A.Br.var.stelipila MAXIM.) was extracted with methanol and the methonolic extract was extracted with ether. The insoluble part was further extracted with ethyl acetate and the latter extract afforded a new flavonoid glycoside as pale yellow needles, mp 256-257°, in 0.3% yield. This glycoside corresponded to the molecular formula of C21H20O10·H2O. Its hydrolysis with conc.hydrochloric acid afforded one mole each of scutellarein (5, 6, 7, 4'-tetrahydroxyflavone) and rhamnose. This is a new glycoside and was named sorbarin. Hydrolysis of the thoroughly methylated compound of sorbarin gave an aglycone of mp 197°, which was identified with scutellarein 5, 6, 4'-trimethyl ether, mp 198°, obtained by hydrolysis of the thoroughly methylated compound of pectolinarin. Consequently, sorbarin was determined as scutellarein 7-momorhamnoside.抄録全体を表示PDF形式でダウンロード (383K) -
吉柳 節夫, 井口 定男1969 年 89 巻 5 号 p. 707-711
発行日: 1969/05/25
公開日: 2008/05/30
ジャーナル フリーTo obtain basic data on crystallization of the molecular compound of aminopyrine and barbital from aqueous solution, the diagram of the ternary system, aminopyrine-barbital-water, was studied in the temperature range 0° to 98°. It was observed that lower critical temperature of layering of the aminopyrine-water system decreases with addition of barbital, that concentration ranges of aminopyrine and barbital in the solution which is in equilibrium with the molecular compound crystals, are narrowed with decrease of temperature and that concentration of barbital decreases more rapidly than that of aminopyrine. Therefore the best conditions to obtain the molecular compound are as follows : 1) excess amount of aminopyrine, 2) crystallization from concentrated solution, and 3) crystallization at high temperature. Furthermore, crystals of the molecular compound were examined by X-ray diffraction measurement; they belong to monoclinic system and the unit cell dimensions are : a 11.92, b 26.92, c 7.20 Å, β 97.3, with Z=4, space group is P21/c.抄録全体を表示PDF形式でダウンロード (619K) -
高木 敬次郎, 柴田 丸1969 年 89 巻 5 号 p. 712-720
発行日: 1969/05/25
公開日: 2008/05/30
ジャーナル フリーCrude saikosides are crude saponin fraction extracted from Bupleurum falcatum L. some pharmacological properties, particularly the acute toxicity ana the central depressant action of this fraction were described. Crude saikosides showed a strong toxic effect by intraperitoneal administration but low toxicity by oral route. High hemolytic value was obtained with this crude saponin. Crude saikosides had potent sedative, analgesic, hypothermic and antipyretic effect. Furthermore they had a potent antitussive effect. On the other hand they did not show any anticonvulsant activity nor reduction of muscle tone using the grip strength test. From these findings it may be concluded that crude saikosides have a strong central depressant action.抄録全体を表示PDF形式でダウンロード (982K) -
亀谷 哲治, 野口 功1969 年 89 巻 5 号 p. 721-725
発行日: 1969/05/25
公開日: 2008/05/30
ジャーナル フリーTreatment of 7-benzyloxy-1-(3-benzyloxy-4, 5-dimethoxybenzyl)-6-methoxy-1, 2, 3, 4-tetrahydroisoquinoline (III) with acetic acid and 37% formaldehyde solution resulted in the progress of the Mannich reaction and protoberberine bases (VI and VII) were obtained. These bases were identified with the authentic sample obtained by the treatment of the hydrochloride of III with 37% formaldehyde solution. Debenzylation of VI and VII gave the phenolic bases, X ((±)-O-demethylstepharotine) and XI, and their methylation with diazomethane gave the same (±)-O-methylstepharotine (XII). XI was also obtained by debenzylation of III to IX and its Mannich reaction. The Eschweiler-Clarke reaction of III gave VI and VII accompanied by a small amount of 7-benzyloxy-1-(3-benzyloxy-4, 5-dimethoxybenzyl)-6-methoxy-2-methyl-1, 2, 3, 4-tetrahydroisoquinoline (VIII) which was identified with an authentic specimen.抄録全体を表示PDF形式でダウンロード (614K) -
岩城 利一郎, 石河 醇一, 工藤 善隆, 入倉 勉1969 年 89 巻 5 号 p. 726-729
発行日: 1969/05/25
公開日: 2008/05/30
ジャーナル フリーEffect of 15 kinds of pharmaceutics acting on the circulatory system, including ATP, nitroglycerin, 4, 4'-diethylaminoethoxyhexostrol, and adrenaline, was examined by their intra-arterial and intravenous injection, to see their effect on the amount of blood flow in coronary circulation, brain, kidneys, intestine, and hind leg circulation system, and systemic blood pressure. Results are listed in Table I.抄録全体を表示PDF形式でダウンロード (578K) -
滝浦 潔, 山本 稔, 辻本 信子1969 年 89 巻 5 号 p. 730-733
発行日: 1969/05/25
公開日: 2008/05/30
ジャーナル フリーUronic acid forms a complex salt with molybdic acid in acetic acid and this complex shows rotatory dispersion curve with a maximum rotation value at 345 mμ. When molybdic acid is added to uronic acid lactone, a considerable time is required until the optical rotation reaches a constant value. There is a proportional relation between the degree of optical rotation at 345 mμ and concentration of uronic acid, and uronic acid can be determined by using this relationship.抄録全体を表示PDF形式でダウンロード (434K) -
正田 芳郎, 橋本 圭二, 井上 武久, 沢田 徳之助1969 年 89 巻 5 号 p. 734-736
発行日: 1969/05/25
公開日: 2008/05/30
ジャーナル フリーQuantitative determination of glucose and fructose in honey was carried out by gas chromatography. This new method was found to be much more rapid and simple than the existing colorimetry, gravimetry, or microbiological assay, and would be of advantage in the quality control of honey. Trimethylsilylation of glucose and fructose was examined by using trimethylchlorosilane, hexamethyldisilazane, N, O-bis (trimethylsilyl) acetamide, and N-trimethylsilylimidazole.抄録全体を表示PDF形式でダウンロード (398K) -
富田 真雄, 沢田 徳之助, 小塚 睦夫, 浜野 大助, 吉村 克巳1969 年 89 巻 5 号 p. 737-740
発行日: 1969/05/25
公開日: 2008/05/30
ジャーナル フリーLaurolitsine (II) was isolated from the root of a Lauraceous plant, Lindera strychnifolia (SIEB. et ZUCC.) F.VILL. (Japanese name "Tendai -uyaku"). Launobine (V) was isolated from the bark and wood of Lindera umbellata THUNB. (Japanese name "Kuromoji").抄録全体を表示PDF形式でダウンロード (600K) -
山名 月中, 水上 勇三, 辻 彰, 市村 藤雄1969 年 89 巻 5 号 p. 740-744
発行日: 1969/05/25
公開日: 2008/05/30
ジャーナル フリーDegradation of hydrochlorothiazide (I) and N, N'-dimethylhydrochlorothiazide (IV) at pH 1.5-11.5 in aqueous solutions at 90° and 60° was examined. The pH rate profiles with bell-shaped curves at neutral pH region were obtained from the kinetic measurements. I and IV were found to be most stable at pH 2.5 and 8.0, respectively.抄録全体を表示PDF形式でダウンロード (491K)
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