巻号一覧
79 巻, 5 号
選択された号の論文の35件中1～35を表示しています
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スルホニルウレア系化合物の合成大西 定夫1959 年 79 巻 5 号 p. 559-566
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリーA derivative of sulfonylurea, 1-p-tolylsulfonyl-3-butylurea (D-860), is generally used as a hypoglycemic drug for oral administration. A process for the syntheses of sulfonylurea and sulfonylthiourea was considered and a new method whereby D-860 is obtained in economically advantageous manner via sulfonylthiourea was established. The reaction is effected by heating potassium salt of toluenesulfonamide and butyl isothiocyanate in benzene system solvent and 1-p-tolylsulfonyl-3-butylthiourea so formed is oxidized with hydrogen peroxide. The yield is extremely good, being 95% calculated from the sulfonamide. About 90 kinds of the derivatives of these compounds were also prepared by the same process.抄録全体を表示PDF形式でダウンロード (1059K) -
2-Mercapto-3-hydrazinoquinoxalineについて浅野 和夫, 浅井 外夫1959 年 79 巻 5 号 p. 567-571
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリーSome physicochemical properties of 2-mercapto-3-hydrazinoquinoxaline are described. Examinations were made on the α- and β-form crystals of this compound, described in Part III of this series, on conditions for their formation, state of decomposition during heating, measurement of ultraviolet and infrared absorption spectra, molecular weight, X-ray diffraction pattern, coloration to nitroprusside during heating, antibacterial action, and variation in ultraviolet absorption. There was a slight difference between the two forms and such a difference was thought to be due merely to the difference in crystal behavior. Decomposition with acid produced 2, 3-dihydroxyquinoxaline, while that with alkali was found to produce an unknown seven-membered ring compound, 6, 7-dihydrodiquinoxalo [2, 3-b, 2′, 3′ -f]-1, 4, 5-thiadiazepine.抄録全体を表示PDF形式でダウンロード (751K) -
ジギタリス・プルプレアのB系配糖体とJensenの螢光定量用試薬の反応成績体 その1濾紙クロマトグラフィーによる研究笹川 義郎1959 年 79 巻 5 号 p. 571-574
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリーDetermination of glycosides having no deoxysugar, such as digitalinum verum and strospeside, with Jensen's reagent always gives a value higher than the theoretical one for the first several hours. To make the cause clear, gitoxigenin, strospeside, purpurea glycoside B, digitalinum verum, and gitorin were allowed to react with Jensen's reagent, and the products were investigated by paper chromatography at regular intervals during the reaction.抄録全体を表示PDF形式でダウンロード (1018K) -
ジギタリス・プルプレアのB系配糖体とJensenの螢光定量用試薬の反応成績体その2 Digitalinum verumまたはStrospesideとJensenの螢光定量用試薬との反応中間生成物について笹川 義郎1959 年 79 巻 5 号 p. 575-578
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリーIntermediates in the reaction of digitalinum verum or strospeside with Jensen's reagent for determination of B series glycosides of Digitalis purpurea L. were isolated and identified as their Δ14, 16-dianhydro derivatives. The fluorescence of solutions of these substances was found to be stronger than that of a solution in the same concentration of Δ14, 16-dianhydrogitoxigenin. Thus, it was found that the reason why determination of digitalinum verum and strospeside with Jensen's reagent gave values higher than the theoretical one for the first several hours is due to the formation of such intermediates.
It was also found that there are two groups in the B-series glycoside of Digitalis purpurea L., one of which is first hydrolized by Jensen's reagent to gitoxigenin and then dehydrated to Δ14, 16-dianhydrogitoxigenin, while the other is first dehydrated by the reagent to Δ14, 16-dianhydroglycosides and then hydrolized to Δ14, 16-dianhydrogitoxigenin. Consequently, in the latter case, if the determination is conducted in the presence of Δ14, 16-dianhydroglycoside, a value higher than theoretical one is obtained, because the fluorescence of Δ14, 16-dianhydroglycosides is stronger than that of Δ14, 16-dianhydrogitoxigenin.
It is necessary, therefore, to effect the determination after Δ14, 16-dianhydroglycoside has changed into Δ14, 16-dianhydrogitoxigenin.抄録全体を表示PDF形式でダウンロード (1099K) -
Bis (ethylmercuric) Sulfideの薬理的研究加来 天民, 高崎 能邦, 由井薗 倫一, 本山 和子1959 年 79 巻 5 号 p. 579-582
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリーAcute toxic symptoms of bis (ethylmercuric) sulfide include central paralysis as the chief conditions, with lowering of respiration, heart action, and blood pressure, death occurring through paralysis of respiratory nerves. In chronic toxicity, there occurs damage to the liver, kidneys, heart, and lungs. There is no marked difference in toxicity according to different alkyl, aryl, and aralkyl groups but diethylmercury is less toxic than its sulfide. The cause of chronic toxicity is assumed to be the concerted action of the sulfide and biological decomposition product, diethylmercury.抄録全体を表示PDF形式でダウンロード (746K) -
マムシ毒レシチナーゼAのカラムクロマトグラフィー岩永 貞昭, 河内 佐十1959 年 79 巻 5 号 p. 582-586
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリーThe poison of Japanese asp (Agkistrodon halys blomhoffi BOIE) contains two kinds of lecithinase A, one of which is adsorbed on anion exchange cellulose and the other is not. These lecithinases can be separated by column chromatography using diethylaminoethylcellulose. The lecithinase A-I, eluted by 0.005M acetate buffer (pH 6.0) is considered to be a basic protein, and the lecithinase A-II eluted by 0.2M acetate buffer (pH 6.0), a nearly neutral protein.抄録全体を表示PDF形式でダウンロード (1172K) -
藤村 一, 大幡 勝也, 川井 清尚, 疋田 英昭, 杉井 通泰1959 年 79 巻 5 号 p. 587-591
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリーMethyl, benzyl, and phenyl derivatives of 2-diethylaminoethyl 2-(ar-β-tetralyl) glycolate were prepared in order to submit them to pharmacological examination. These compounds failed to show any better properties than Benactyzine Hydrochloride in the point of toxicity, analgesic action, potentiation effect on methylhexabital hypnosis, effect on body temperature, and spasmolytic action but the benzyl and phenyl derivatives indicated an excellent effect in local anesthetic action, the phenyl derivative showing about one-half the effect of Dibucaine. Introduction of ar-β-tetralyl group in place of one phenyl ring in Diphenhydramine or its thio derivative was found to show a marked potentiation of the local anaesthetic action of these compounds and the same tendency was found in the present series of experiments.抄録全体を表示PDF形式でダウンロード (775K) -
中川 俊夫, 森 芳夫1959 年 79 巻 5 号 p. 591-595
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリーOf the medicinal drugs sparingly soluble in water, those possessing hydroxyl radical can be converted to water-soluble derivatives by the following two methods.
1) Esterification of the drugs by treatment with methoxypolyoxyethylene-acetyl or -propionyl chloride to obtain respective -acetate or -propionate.
2) The reaction of chloroacetates of the drug with sodium methoxypolyoxyethylene-acetate or -propionate to obtain methoxypolyoxyethylene-acetoxyacetate or -propionyl-oxyacetate.
Water-soluble derivatives of vitamin E, hydrocortisone, prednisolone, hexestrol, and diethylstilbestrol were obtained by the first method, and those of vitamin E, testosterone, β-estradiol, and hexestrol by the second method. The potency of these derivatives differed from that of the parent compound.抄録全体を表示PDF形式でダウンロード (804K) -
Benzylidene-d-sorbitolのゲル化遠藤 文男1959 年 79 巻 5 号 p. 595-598
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリーWhen a solution of benzylidene-d-sorbitol in various solvents, dissolved with warming, is allowed to cool, a jelly-like gel is formed. In order to clarify this gelation phenomenon, the three kinds of mono-, di-, and tri-compounds of benzylidene-d-sorbitol were submitted to separation and purification. It was thereby found that there is some difference in these three compounds on the behavior to solvents and the degree of gelation, but they all did have the ability to form a gel. Solubility of these compounds in ethanol and benzene, which are representative solvents for gelation, and limit concentration for gelation, as well as the properties of the gel formed, were examined.抄録全体を表示PDF形式でダウンロード (615K) -
多価アルコール及びその関連化合物のBenzylidene誘導体のゲル化能遠藤 文男1959 年 79 巻 5 号 p. 598-600
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリーBenzylidene-d-sorbitol undergoes gelation in various solvents and examinations were made to see if polyhydric alcohols other than sorbitol and related compounds would also show such ability. It was found that xylitol, having configuration similar to d-sorbitol, was also capable of undergoing gelation.抄録全体を表示PDF形式でダウンロード (479K) -
諸種のアルデヒドとd-Sorbitolとの縮合物のゲル化能遠藤 文男1959 年 79 巻 5 号 p. 600-602
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリーBenzylidene-d-sorbitol tends to form a jelly-like gel in various organic solvents. Compounds similar to benzylidene-d-sorbitol were prepared with ring-substituted aliphatic aldehydes and other carbonyl compounds in place of benzaldehyde condensed with d-sorbitol and the ability of these compound to undergo gelation was examined. It was thereby found that m-nitro-, m-chloro-, and p-bromo-benzylidene-d-sorbitols had weak ability to form a gel but others did not show any such capacity.抄録全体を表示PDF形式でダウンロード (477K) -
Benzylidene-d-sorbitol及びその関連化合物のゲル化能と溶媒の関係遠藤 文男1959 年 79 巻 5 号 p. 603-606
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリーThe ability of benzylidene-d-sorbitol and related compounds to undergo gelation in various solvents differ according to the kind of solvent. In order to ascertain this point, solubility and degree of gelation of mono-, di-, and tri-benzylidene-d-sorbitol in various solvents were examined but there seemed to be no uniform regularity. It was found that, in general, the solubility is greater in solvents with greater polarity, and, in solvents of the same series, the greater the solubility, the more easily the gelation occurred.
With related compounds, greater solubility in polar solvents was the same as above but there were no regularity in relationship between solubility and gelation. Consequently, gelation is based on the properties of the compound itself while the compounds capable of undergoing gelation have different capacity according to the kind of solvent.抄録全体を表示PDF形式でダウンロード (607K) -
ゼリー中の拡散速度とゼリーの硬さ遠藤 文男1959 年 79 巻 5 号 p. 606-608
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリーVarious solvents undergo gelation by the action of dibenzylidene-d-sorbitol to form a jelly, and the hardness of jelly and diffusion rate of dye in this jelly were comparatively measured. It was found that there is approximate parallelism between these two factors. Since the hardness of jelly is affected by viscosity of that solvent, relationship with viscosity was also examined. It was thereby learned that an approximate parallelism existed between hardness and square root of viscosity.抄録全体を表示PDF形式でダウンロード (395K) -
えぞばいけい草の成分清水 文治, 鈴木 稔1959 年 79 巻 5 号 p. 609-615
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリーEffective principles of domestic Veratrum plants were examined and veratroyl-zygadenine (B-base) and zygacine were isolated from Veratrum oxysepalum TURCZ. from the Hokkaido area. It has been proved now that the effective principle in domestic Veratrum plants has a zygadenine as the skeleton. As an accompanied base, rubijervine was isolated from Veratrum oxysepalum.抄録全体を表示PDF形式でダウンロード (1270K) -
ばいけい草の成分清水 文治, 林 了三1959 年 79 巻 5 号 p. 615-618
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリーEffective principles of domestic Veratrum plants were examined and zygacine (3-acetylzygadenine) was isolated as the chief component from Veratrum grandiflorum LOESEN from Nagano Prefecture in central part of Japan.抄録全体を表示PDF形式でダウンロード (623K) -
こばいけい草の成分鈴木 稔, 村瀬 安弘, 林 了三, 三瓶 信良1959 年 79 巻 5 号 p. 619-623
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリーEffective principle of domestic Veratrum plants was examined and angeloylzygadenine was isolated as the chief component from Veratrum album Staminium MAXIM. growing in Nagano Prefecture.抄録全体を表示PDF形式でダウンロード (971K) -
非対称型ケトンに対する義酸エチルエステルの作用位置決定への応用について安田 博幸1959 年 79 巻 5 号 p. 623-627
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリーWhen ethyl formate is applied to unsymmetrical ketones with a general formula of RCH2COCH2R′, the question is which of the two active methylenes on either side of the carbonyl would be formylated. The α-formyl-ketones so formed was reacted with hydroxylamine to form 4, 5-disubstituted isoxazoles and this was cleaved by the action of sodium ethoxide to form α-cyano-ketones. The difference in the position of the formyl group in the original α-formyl-ketones would give result in the structural difference of α-cyano-ketones finally formed and this reaction was utilized as the new method for determining the action point of ethyl formate on unsymmetrical ketones. This reaction is effected in few steps, the yield is good, and characterization is easy. The action site of ethyl formate was determined in eight kinds of unsymmetrical ketones and relationship to the structure of ketones was also examined.抄録全体を表示PDF形式でダウンロード (934K) -
スルホニルウレア系化合物の血糖値測定法大西 定夫1959 年 79 巻 5 号 p. 628-631
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリーIn order to examine the hypoglycemic action of the compounds of sulfonylurea series previously synthesized, variation of blood sugar level was examined using albino rats, with oral administration of D-860 as a standard and of water as the control. The difference of the group treated with D-860 from the control was proved highly significant after comparison of mean values of blood sugar and the further stochastical analysis. In the light of these data, it was found reasonable to examine the hypoglycemic activity of each sample by this method.抄録全体を表示PDF形式でダウンロード (438K) -
スルホニルウレア系化合物の血糖降下作用大西 定夫1959 年 79 巻 5 号 p. 632-636
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリーAbout 60 kinds of the compound of sulfonylurea series whose synthesis has been reported were examined for hypoglycemic action, using albino rats and several of these compounds were found to be comparable to D-860. One of these, 1-p-toluenesulfonyl-2-allylurea, was found to have a fairly strong action. A certain amount of conclusion was drawn regarding relationship between chemical structure and hypoglycemic action of these compounds. Sulfonylthiourea derivatives were almost devoid of hypoglycemic action but they are now being examined for other pharmacological activities.抄録全体を表示PDF形式でダウンロード (553K) -
川谷 豊彦, 藤田 早苗之助, 久保木 憲人, 青柳 喜典1959 年 79 巻 5 号 p. 637-639
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリー1) As a trial cultivation of Atropa Belladonna L. in Japan, five strains of foreign origin were cultivated at Kasukabe Experiment Station of Medicinal Plants, and yield of leaves and roots, and content of total alkaloid were examined with the secondyear growth, comparing these values among the five strains.
2) Yield of air-dried leaves per plant was 31.94-64.22g., an average of 53.176g., which was better than that in the original habitat (cf. Table I). There was no significant difference among the strains (cf. Table I).
3) Yield of air-dried roots per plant was 13.2-81.6g., an average of 37.12g., which was comparable to that in the original habitat (cf. Table II). There was a very highly significant difference among the strains (Table III) but no significant effect was found in harvesting of leaves on the yield of roots (Table III).
4) The content of total alkaloid (as hyoscyamine) in the root was 0.535-0.915%, an average of 0.704%, which was better than that in the original habitat (Table IV). There was a highly significant difference among the strains. It was stochastically proved that harvesting of leaves effected decrease of the content of total alkaloid in the root (Table V).抄録全体を表示PDF形式でダウンロード (459K) -
体温降下作用について その2北川 晴雄, 岩城 利一郎1959 年 79 巻 5 号 p. 639-643
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリーA thiocoumarin derivatives, an aminocoumarin derivative, a coumarin homolog, eight derivatives of coumarin-carboxylic acid, seven derivatives of halogenated coumarin, and three derivatives of 3-substituted 4-hydroxycoumarin were examined for hypothermic action, using rats, and structure-activity relationship was further clarified.
1) 2-Thiocoumarin and 6-chloro-2-thiocoumarin, a derivative of 6-chlorocoumarin which have comparatively strong effect, had only a weak effect.
2) 6-Aminocoumarin hydrochloride has a strong effect but the action was not potentiated by derivation to a salicylate.
3) Chromone-2-carboxylic acid had weaker effect than chromone but did not have such strong toxicity as coumarin-3-carboxylic acid.
4) Of the salts of coumarin-3-carboxylic acid with aniline, phenetidine, 6-amino-coumarin, and 4-methyl-7-aminocoumarine, and acid amides with ammonia, aniline, phenetidine, and 6-aminocoumarin, the salt with 6-aminocoumarin had the strongest action with longest duration of the effect.
5) Of the halogenated coumarins, those with chlorine in 3- and 6-position had a strong activity, while introduction of a methyl in 4-position weakened the activity.
6) In derivatives of 4-hydroxycoumarin condensed with aldehydes at 3-position, the vanilin condensate had the strongest effect, while those formed by condensation with chloral hydrate and antipyrine-4-aldehyde had effect similar to that of 4-hydroxycoumarin.抄録全体を表示PDF形式でダウンロード (743K) -
Thiourea AdductによるTurmeroneの精製と安定化美間 博之1959 年 79 巻 5 号 p. 644-649
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリーChief components of curcuma oil are turmerone and ar-turmerone which are used as a cholagogic but turmerone has not been extracted in pure state as yet. Turme-rone was therefore extracted as its inclusion compound with thiourea adduct and a pure turmerone was obtained from it. From the physical and chemical properties of turmerone and its derivatives, turmerone seems to have a terminal vinyl group and dienic bonds in and outside the ring. Turmerone has a tendency, when left in the air, to form a dimer with consequent change in its optical rotation but its thiourea adduct is stable and remains unchanged for a period of six months. Turmerone has cholagogic activity in 200mg./kg. dose but the activity decreases by dimerization. The thiourea adduct has a potency corresponding to the amount of turmerone included in it and this adduct formation can be utilized in the manufacture of preparations as a means of obtaining stable crystals without loss of pharmacological activity.抄録全体を表示PDF形式でダウンロード (941K) -
Thiourea Adductの加圧による変化美間 博之1959 年 79 巻 5 号 p. 649-653
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリーInfrared spectrum of isoöctane-thiourea adduct in KBr disk showed that the adduct was already decomposed. In order to examine the assumption of Stewart that thiourea adduct is probably decomposed by compression, thiourea adducts of 10 compounds were prepared and their infrared absorption spectra were measured in KBr disk, examining absorptions at 13.75 and 13.9 μ for the evidence of decomposition. It was thereby found that thiourea adducts other than those of camphor, 9-oxocamphor, turmerone, and decalin underwent decomposition. When KBr disks of these adducts were prepared without evacuation, the disks powdered, and infrared spectra measured in Nujol, decomposition did not occur in adducts other than those of isoöctane and carbon tetrachloride. Since their behavioir towards decomposition is different according to the kind of guest molecule and the decomposition differs according to whether the adduct is pressed under the atomospheric or diminished pressure, this decomposition is not due to destruction of crystal lattice by compression but the liberation of volatile molecules due to degree of evacuation and generation of heat by compression leaving thiourea in rhombic state. The fact that adducts formed from non-volatile compounds do not undergo change on compression was confirmed by thermal analysis. This was also proved by the fact that 9-oxo-camphor-thiourea adduct formed a stable tablet.抄録全体を表示PDF形式でダウンロード (788K) -
2-Sulfonyloxyethyl Sulfone類の抗菌性について石舘 守三, 南原 利夫1959 年 79 巻 5 号 p. 653-658
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリーAs compounds having the ability to sulfonethylate nucleophilic groups, 36 kinds of compound of the general formulae R-SO2CH2CH2OSO2R′ and R-SO2CH2CH2OP(O) (OC6H5)2 (R=CH3, C6H5, p-CH3C6H4, p-CH3CONHC6H4, p-NO2C6H4, 2, 4-(NO2)2C6H3, p-HOOCC6H4, p-CH3OOCC6H4; R′=CH3, C6H5, p-CH3C6H4, p-CH3CONHC6H4, p-ClC6H4, p-BrC6H4) were prepared and their antibacterial action against Mycobacterium tuberculosis, Staphylococcus aureus, and Escherichia coli, and reaction velocity with sodium thiosulfate were examined. In general, these compounds were found to have a fair antibacterial activity against Staph. aureus and E. coli, especially the compound where R is p-nitrophenyl group. It is interesting that the reaction of this compound with sodium thiosulfate is far faster than the other compounds. It was found that the affinity of this series of compounds to SH group is due to the activity of secondary vinyl sulfone group same as in 2-haloethyl sulfones.抄録全体を表示PDF形式でダウンロード (1011K) -
ヒドラジノキノキサリン誘導体の合成 その1浅野 和夫1959 年 79 巻 5 号 p. 658-660
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリーIn order to examine the relationship between chemical structure and antibacterial action in 2-mercapto-3-hydrazinoquinoxaline, 2-hydroxy and 2-methoxy derivatives were prepared. After examining several routes, the compounds were prepared by application of hydrazine respectively to 2, 3-dihydroxy- and 2-methoxy-3-chloro-quinoxaline. The compounds synthesized failed to show any antibacterial action, indicating that the substituent in 2-position must have sulfur. As a part of synthetic method, nitration of 2-hydroxyquinoxaline was examined and it was found that the nitro group is introduced into 7-position.抄録全体を表示PDF形式でダウンロード (585K) -
ヒドラジノキノキサリン誘導体の合成 その2浅野 和夫1959 年 79 巻 5 号 p. 661-663
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリーVariation in antibacterial action was examined with 2-methylthio-3-hydrazino-quinoxaline and 2-mercapto-3-acetylhydrazinoquinoxaline. In the case of 2-methylthio compound, antibacterial activity disappeared entirely and this indicated that the prototropy of 1, 2-position in quinoxaline is necessary for antibacterial activity. In the case of 3-acetylhydrazino compound, changes in antibacterial spectrum in vitro, as previously described, were found to take place. Triazoloquinoxaline was prepared from 3-acetylhydrazino derivative.抄録全体を表示PDF形式でダウンロード (498K) -
Alkyl 2-Alkoxymethylene-3-alkoxypropionateの検討高見沢 映, 徳山 幹治, 佐藤 久夫1959 年 79 巻 5 号 p. 664-669
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリーMethylation of ethyl 2-sodioformyl-3-ethoxypropionate (VIII), obtained by formylation of ethyl 3-ethoxypropionate (VII), afforded ethyl 2-methoxymethylene-3-ethoxypropionate (IX) which was derived to ethyl 2-methoxyethoxymethyl-3-ethoxypropionate (X) and ethyl 2-methoxyethoxymethylacrylate (XI). It was found that a correlation similar to that in 2-alkoxypropionitriles described previously, existed among these three compounds. Both (IX) and (X) were found to react with acetamidine to form 2-methyl-4-hydroxy-5-ethoxymethylpyrimidine (XIII) in both cases, and there was no difference between the acetal and enol-ether compounds in this reaction, contrary to the case of the corresponding 3-alkoxypropionitriles reported before.抄録全体を表示PDF形式でダウンロード (837K) -
2-Methoxyethoxymethyl-3-ethoxypropionitrileおよびEthyl 2-Methoxyethoxymethyl-3-ethoxypropionateと液安との反応について高見沢 映, 徳山 幹治1959 年 79 巻 5 号 p. 670-673
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリーReaction of methyl acetimidate to the reaction product of 2-methoxyethoxymethyl-3-ethoxypropionitrile (I) and liquid ammonia, followed by treatment with hydrochloric acid results in the formation of 2-methyl-4-amino-5-ethoxymethyl-pyrimidine (IV). This shows the formation of 2-aminomethylene-3-ethoxypropionitrile (III) as an intermediate of this reaction. Similar reaction of ethyl 2-methoxyethoxymethyl-3-ethoxypropionate (VI) also shows the formation of ethyl 2-amino-methylene-3-ethoxypropionate (VII) as an intermediate. A new reaction was thereby found that the acetal group changes into aminomethylene group by reaction with liquid ammonia. In the case of reaction between ethyl 2-methoxymethylene-3-ethoxypropionate (IX) and liquid ammonia, a mixture of ethyl 2-aminomethylene-3-ethoxypropionate (VII) and 2-aminomethylene-3-ethoxypropionamide (X) is produced intermediately and this is further derived to 2-methyl-4-hydroxy-5-ethoxymethyl-pyrimidine (VIII) through imidic ester.抄録全体を表示PDF形式でダウンロード (582K) -
3-Aminopropionitrile誘導体の合成およびその反応について高見沢 映, 徳山 幹治1959 年 79 巻 5 号 p. 674-678
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリーReaction of 2-diethoxymethyl-acrylonitrile (V) with liquid ammonia produces 2-diethoxymethyl-3-aminopropionitrile (VI), with formation of bis (3-cyano-3-diethoxymethylethyl) amine (VII) as a by-product. (VI) undergoes reaction with acetamidine in ethanol to form 2, 7-dimethyl-5, 6-dihydropyrimido[4, 5-d]pyrimidine (XIII) as an intermediate, as in the case of 2-methoxyethoxymethyl-3-ethoxypropionitrile (IV), and its hydrolysis results in formation of 2-methyl-4-amino-5-acetamidomethylpyrimidine (XIV) in a good yield. The 3-acetamido compound, however, does not react with acetamidine under identical reaction conditions.抄録全体を表示PDF形式でダウンロード (706K) -
黄血塩-赤血塩混合規定液による金属塩の分極沈殿滴定について榎 健寿, 森坂 勝昭, 原田 多賀子, 角谷 暢子1959 年 79 巻 5 号 p. 679-683
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリーWhen potassium ferricyanide or ferrocyanide reacts with metal ion to form a precipitate, the solubility product of ferro-metal salt is generally smaller than that of ferri-metal salt. In such a case, the use of a ferricyanide-ferrocyanide mixture would result in preferential precipitation of a ferro salt. Consequently, a polarographic titration of various metals with normal solution of ferrocyanide-ferricyanide mixture was carried out and it was found that a determination can be effected according to the normality of the ferrocyanide in the mixed solution. Some of the metals were found to be determined by the normality of the ferrocyanide-ferricyanide mixture.抄録全体を表示PDF形式でダウンロード (699K) -
a) 17α位水酸基のアセチル化の20位カルボニル基の反応性に及ぼす影響 b) 17位カルボニル基ならびに20位カルボニル基と5,6α-エポキシ基の反応性の比較和田 俊洋1959 年 79 巻 5 号 p. 684-687
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリーIt was found that the esterification of hydroxyl group in 17α-position of pregnane series compounds resulted in loss of activity, the carbonyl at 20-position not reacting with the Girard-T reagent, sodium borohydride, and ethylene glycol. Difference in ease or difficulty in reduction of carbonyl group in 17-position of androstane series and 20-position of pregnane series, and 5, 6α-epoxy group with sodium borohydride in ethanol was examined and the carbonyl group was found to be reduced preferentially over the epoxy group.抄録全体を表示PDF形式でダウンロード (572K) -
Callicreinの等電点について守屋 寛, 島沢 英一郎1959 年 79 巻 5 号 p. 688-690
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリーIt was shown in Part III of this series, that purification by zone electrophoresis afforded a homogeneous callicrein (product L, 570U/mg.) from hog pancreas. The isoelectric point of this homogeneous callicrein was measured in order to elucidate its physical and chemical properties. The method of paper electrophoretic analysis, reported by Kunkel and Tiselius, which enables measurement of a micro-quantity, was used. Dextran, which is considered to be in uncharged state, was run with callicrein in order to correct the migration distance of callicrein. This result showed that the isoelectric point of homogeneous callicrein obtained from hog pancreas is at around pH 2.4. For staining of dextran, a 1% ethanolic solution of bromphenol blue is used and stained sample is washed by drops of ethanol.抄録全体を表示PDF形式でダウンロード (791K) -
富田 真雄, 松村 寿賀子1959 年 79 巻 5 号 p. 690-692
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリーApplication of metallic sodium to tetrahydroberberine (I) in liquid ammonia is known to result in the cleavage of methylenedioxy group, accompanied by secondary reaction of demethylation of methoxyl in 9-position on the ring. The same decomposition with sodium in liquid ammonia was carried out on tetrahydropalmatine (IV) and tetrahydrojatrorrhizine (VI), and both compounds were found to undergo demethylation at 9-position of the tetrahydroberberine ring, where a new phenolic hydroxyl is formed, resulting in the formation of tetrahydropalmatrubine (V) from (IV), and (VII) from (VI).抄録全体を表示PDF形式でダウンロード (605K) -
Androgenのエポキシ化および飽和化によるAndrogenic ActivityとProtein Anabolic Activityの変化について和田 俊洋1959 年 79 巻 5 号 p. 693-695
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリーEpoxidation of the double bond in 3-oxo-4-androstene and 3β-hydroxy-5-androstene results in loss of both androgenic and protein anabolic activities by subcutaneous injection. Saturation of double bond in 19-nor compounds results in weakening of the two activities but androgenic activity is more greatly diminished in 17β-hydroxy-19-norandrostan-3-one. Progestational activity also diminishes in 17α-methyl-17β-hydroxy-19-norandrostan-3-one.抄録全体を表示PDF形式でダウンロード (538K) -
エストラジオール-17βの新製法和田 俊洋1959 年 79 巻 5 号 p. 696-697
発行日: 1959/05/25
公開日: 2010/02/19
ジャーナル フリーUrushibara and Chuman prepared metallic nickel by utilization of difference in ionization by adding zinc dust or aluminum to aqueous solution of nickel salts. Using this nickel as a catalyst, they prepared estradiol-17β (II) from estrone (I) by reduction of its alkaline solution with zinc dust or aluminum. In the present series of work, metallic copper was prepared from aqueous solution of copper salt by the same procedure and, using this copper as a catalyst, (I) was reduced with zinc dust or aluminum from its alkaline solution and (II) was obtained in 80% yield.抄録全体を表示PDF形式でダウンロード (774K)
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