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Akira Takamizawa, Kentaro Hirai
1964 Volume 12 Issue 4 Pages
393-397
Published: April 25, 1964
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The reaction of 3-ethoxy-2-methoxymethylenepropionitrile (I) with various kind of amidine gave 2-alkyl (aryl)-4-amino-5-ethoxymethylpyrimidine derivatives. The reaction of 3-ethoxy-2-methoxyethoxymethylpropionitrile (III) with various amidine derivatives afforded 2, 7-dialkyl (aryl)-5, 6-dihydropyrimido [4, 5-d] pyrimidine, which was converted into 2-alkyl (aryl)-4-amino-5-acylaminomethylpyrimidine. The reaction with ethyl 3-ethoxy-2-methoxymethylenepropionate (VI) or ethyl 3-ethoxy-2-ethoxymethoxymethyl-propionate (XXIV) yielded 2-alkyl (aryl)-5-ethoxymethyl-4-pyrimidinol. 2-Phenyl derivative (XXI) was converted into 4-amino compound through 4-chloro compound.
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Akira Takamizawa, Yoshiro Sato
1964 Volume 12 Issue 4 Pages
398-403
Published: April 25, 1964
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On the reaction of potassium O-ethyl thiocarbonate (I) or potassium O-ethyl dithiocarbonate (IV) with phosphorus trichloride, tris (ethoxycarbonyl) phosphorotrithioite (IIa) or tris (ethoxythiocarbonyl) phosphorotrithioite (V) were synthesized, respectively. From the treatment of IIa or V with ethyl chloroformate, the same product, diethyl ethoxy-carbonylphosphite (IIIa), accompanied by carbonyl sulfide and ethyl chloride from IIa, and carbon disulfide and ethyl chloride from V, were given in high yield. When tris (alkoxycarbonyl) phosphorotrithioite (II) and thiamine sodium salt (VII) were reacted together, O, S-bis (alkoxycarbonyl) thiamine (IX) was produced. On the other hand, from the reaction of dialkyl ethoxycarbonylphosphite with VII, O, S-bis (ethoxycarbonyl)-thiamine (IXa) was also obtained, but in this cases S-alkylthiamines were main products.
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Kunio Nakagawa, Kenichi Igano, Jitsuo Sugita
1964 Volume 12 Issue 4 Pages
403-407
Published: April 25, 1964
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Solid nickel peroxide, readily obtainable by the treatment of nickel salts with sodium hypochlorite in alkaline solution, has been proved to be an useful reagent for the oxidative cleavage of α-glycols and α-hydroxy acids in aprotic solvents. Some kinds of aldehydes or ketones were obtained in moderately good yield as glycol cleavage products. With nickel peroxide in an aqueous alkaline solution, α-keto alcohols and α-keto acids were transformed into carboxylic acids by the oxidative cleavage.
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Shojiro Uyeo, Yoshitomo Yamamoto, Tsunehiro Kitagawa
1964 Volume 12 Issue 4 Pages
408-412
Published: April 25, 1964
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Oxidation of α-deoxydihydrolycorenine (I) with potassium dichromate in sulfuric acid gave α-dihydrohomolycorine and with potassium permanganate α-deoxydihydro-2-oxolycorenine (V) which reverted to I on treatment with lithium aluminum hydride. β-Deoxydihydrolycorenine (II) gave with potassium permanganate β-dihydrolycorenine together with β-dihydrohomolycorine which constituted the sole product of dichromate oxidation of (II) and gave on further oxidation with permanganate the N-formyl derivative (XII) which was converted into β-dihydro-7-oxopluviine (XI) on treatment with alcoholic sodium hydroxide. α-Dihydrolycorenine (XIII) was obtained only by reduction of α-dihydrohomolycorine with lithium aluminum hydride under controlled conditions.
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Tamotsu Koizumi, Takaichi Arita, Kiichiro Kakemi
1964 Volume 12 Issue 4 Pages
413-420
Published: April 25, 1964
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Kinetical mechanism of absorption of sulfonamides through the lipoid barrier is described. Assuming permeation of the drug through the barrier to be governed by three processes, namely, 1) transfer of a drug from the solution to the membrane surface, 2) transfer back to the solution from the surface, and 3) diffusion into the barrier, relationship of absorption rate and partition coefficient are obtained. And that was supported by the experimental data obtained.
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Tamotsu Koizumi, Takaichi Arita, Kiichiro Kakemi
1964 Volume 12 Issue 4 Pages
421-427
Published: April 25, 1964
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Rat small intestine was recirculated in situ with seventeen kinds of sulfonamide and five N
4-acetyl derivatives, and absorption rate of the unionized drug was determined. The kinetical model proposed for the absorption of the drug from rat stomach also accounts for the absorption from rat small intestine, though the organic solvents that give suitable P are different.
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Tamotsu Koizumi, Takaichi Arita, Kiichiro Kakemi
1964 Volume 12 Issue 4 Pages
428-432
Published: April 25, 1964
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Kinetic mechanism of excretion of passively transported sulfonamide from kidney is described. Urinary excretion rate of the drug was determined after oral administration to man. Some of the data obtained fit the mechanism proposed. And drugs which did not fit the mechanism were revealed to participate in the active transport.
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Jiro Kinugawa, Michihiko Ochiai, Chikashi Matsumura, Hiroichi Yamamoto
1964 Volume 12 Issue 4 Pages
433-440
Published: April 25, 1964
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2-Thiocyanatoimidazoles, 3-thiocyanato-1, 2, 4-triazoles, and 1-(4-thiocyanatophenyl)-pyrazoles were synthesized. Antifungal activity of these compounds was examined. Some of 3-thiocyanato-1, 2, 4-triazoles and 1-(4-thiocyanatophenyl) pyrazoles showed highly antifungal activity.
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Minoru Sekiya, Noboru Yanaihara, Mikiaki Tanaka, Minako Saito
1964 Volume 12 Issue 4 Pages
440-444
Published: April 25, 1964
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Acylaminomethylation of aromatic compounds with N, N'-methylenebisamides in acidic media is described. Among the three N, N'-methylenebisamides, i.e., benzamido, acetamido and formamido analogs, the first was the most efficient reagent for the reaction. Benzamidomethylations of aromatic compounds such as 2-naphthol, 4-nitrophenol, benzoic acid, 2-nitrotoluene, 4-nitrotoluene and 2, 4-xylenol were performed.
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Teruji Ishii
1964 Volume 12 Issue 4 Pages
444-449
Published: April 25, 1964
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Eine Apparatur zur Schmelz-und Erstarrungspunktmessung zur Kontrolle fuer Arzneimittel, sowie die Diskussion der mit der vorliegenden Apparatur erzielten Messer-gebnisse bei Proben von WHO-Schmelzpunkt-Referenz-Substanzen wurden angegeben. Die Methode unter Verwendung der vorliegenden Apparatur, welche mit Thermistoren und einer Registriervorrichtung versehen wird, ist dadurch gekennzeichnet, daβ sie es ermoeglicht, aus einer aufgezeichneten thermodynamischen Gleichgewichtskurve den Schmelz-und Erstarrungspunkt einer Substanz objektiv mit groβer Genauigkeit (etwa ±0.2°) zu bestimmen. Die Messung erfolgt mit einer Milligramm-Ordnung der Probe, der man ein entsprechendes, thermisch bestaendiges, indifferentes Zusatzmittel, z.B. Koernchen aus reinem Gold, Quarz, Hartglas oder dgl. zusetzt.
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Yoshihiro Nitta, Minoru Shindo, Keiichi Takamura
1964 Volume 12 Issue 4 Pages
450-453
Published: April 25, 1964
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The methyl steroid-21-yl-β-D-glucopyranosiduronates were prepared by treatment of Reichstein's compound S, cortisone, hydrocortisone, prednisone and prednisolone with methyl 1-bromo-1-deoxy-2, 3, 4-tri-O-acetyl-α-D-glucopyranosiduronate. Treatment of these compounds with methanolic ammonia afforded the corresponding steroid-21-yl-β-D-glucopyranosiduronamide.
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Tyunosin Ukita, Akira Hamada, Mitsuaki Yoshida
1964 Volume 12 Issue 4 Pages
454-459
Published: April 25, 1964
Released on J-STAGE: March 31, 2008
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1-(β-D-Ribofuranosyl) urea (VII) was synthesized via. 2, 3, 5-tri-O-benzoyl-β-D-ribofuranosyl isocyanate (II) and 1-(2, 3, 5-tri-O-benzoyl-β-D-ribofuranosyl) urea (V). One of the intermediate, V, which is an important starting material for the synthesis of ribonucleosides, was obtained in a yield of 70.5% by direct ammonolysis at 0°of the reaction mixture of 2, 3, 5-tri-O-benzoyl-D-ribofuranosyl chloride and silver isocyanate. The structure of V was confirmed by converting it to (β-D-ribofuranosyl) thymine.
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Tyunosin Ukita, Mitsuaki Yoshida, Akira Hamada, Yoshio Kato
1964 Volume 12 Issue 4 Pages
459-465
Published: April 25, 1964
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By condensation of 1-(2, 3, 4, 6-tetra-O-acetyl-β-D-glucopyranosyl) urea (IV) with malonyl chloride in pyridine, N, N'-bis (2, 3, 4, 6-tetra-O-acetyl-β-D-glucopyranosylcarbamoyl)-malondiamide (V) was obtained. This compound, when treated with alkali, afforded each one mole of 1-(β-D-glucopyranosyl) urea and sodium 1-(β-D-glucopyranosyl) barbiturate (VI). Condensation of 1-(2, 3, 5-tri-O-benzoyl-β-D-ribofuranosyl) urea (VII) with malonic acid in acetic anhydride gave N, N'-bis (2, 3, 5-tri-O-benzoyl-β-D-ribofuranosyl-carbamoyl) malondiamide (VIII) with a small amount of 1-(2, 3, 5-tri-O-benzoyl-β-D-ribofuranosyl)-5-acetylbarbituric acid (IX). On alkaline treatment, VIII afforded sodium 1-(β-D-ribofuranosyl) barbiturate (X) and 1-(β-D-ribofuranosyl) urea (XI). The overall yield of VI and X from IV and VII were 30.3% and 37% respectively. The stucture of the glycosylbarbiturates, VI and X, were discussed and their properties were described.
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Keijiro Takagi, Yutaka Kasuya, Kazuo Watanabe
1964 Volume 12 Issue 4 Pages
465-472
Published: April 25, 1964
Released on J-STAGE: March 31, 2008
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A simple and reliable method for production of gastric ulcer on rats by stress was described. Rats fixed on boards were immersed in water of 25°to the depth of xiphoide. After 20 hours, marked gastric erosions were found in the glandular portion of the stomach. This stress is more favourable than other stresses as cold, restraint, or emotional stress by stress box in view of incidence and mortality. Anticholinergics or central depressants effectively inhibited the ulceration and combination of both drugs suppressed it more effectively than single administration of each drug.
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Hiroko Hasegawa, Kyosuke Tsuda
1964 Volume 12 Issue 4 Pages
473-479
Published: April 25, 1964
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9, 10β-Epoxy-9β-estra-1, 4-diene-3, 11, 17-trione (II) and 3, 9α-dihydroxyestra-1, 3, 5 (10)-triene-11, 17-dione (IIIa) was synthesized by the treatment of ⊿
9(11)-estrone (Ia) with perbenzoic acid. 9β-Isomer of IIIa (Va) was obtained from II by the catalytic hydrogenation.
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Yoshio Ueno, Shizuo Suzuki, Ikuko Ueno, Takashi Tatsuno
1964 Volume 12 Issue 4 Pages
479-483
Published: April 25, 1964
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Quant au metabolisme du P. islandicum, nous avons essaye de savoir quel est le meilleur processus de l'activation d'acetate, le systeme de la production de NADPH et la precurseur le plus elementaire des pigments. Nous avons trouve : (1) que l'acetokinase activait l'acetate, (2) que la reaction concernant la G-6-P dehydrogenase pourrait produire le NADPH et (3) que la dose incorporee des precurseurs [
14C] dans la luteoskyrine, (un des pigments obtenus des substances metaboliques du P. islandicum SOPP) augmentait plus specialement quand on avait utilise le sucrose [U-
14C] comme precurseur.
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Shoji Hara, Michiko Takeuchi, Misako Tachibana, Goro Chihara
1964 Volume 12 Issue 4 Pages
483-488
Published: April 25, 1964
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Bile from various animals was submitted directly to thin-layer chromatography, and free and conjugated bile acids and cholesterol in the bile were separated. The chromatogram was analyzed by densitometer with autorecording calculator and animal species difference was revealed by the densitogram. Densitometric analysis gives semiquantitative results and this can be used for clinical chemical analysis.
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Shojiro Uyeo, Hiroshi Irie, Uichiro Kitayama, Tokuyasu Hirose, Akira Y ...
1964 Volume 12 Issue 4 Pages
489-491
Published: April 25, 1964
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Masatake Hori, Isamu Aoki, Satoru Kuwada
1964 Volume 12 Issue 4 Pages
492-494
Published: April 25, 1964
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In the previous investigation on the free amino acid contents in the mycelium of Er. ashbyii, hydroxykynurenine was (+) and proline was (-) in the yellow-type strain and hydroxykynurenine was (-) and proline was (+) in the leuco-type strain. This time the investigation was reexamined with a little different result that hydroxykynurenine was (+) and proline was (+) in the yellow-type strain and hydroxykynurenine was (-) and proline was (+) in the leuco-type strain. Consequently the amino acids were examined more minutely using automatic amino acid analyzer, and from the results shown in the table it was concluded that the characterization of the two strains by the specific amino acids contained in them is unreasonable.
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Zenichi Horii, Masanori Sakamoto, Takefumi Momose, Yasumitsu Tamura
1964 Volume 12 Issue 4 Pages
495-497
Published: April 25, 1964
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Doebner reaction of naphthalene-or 3, 4-dihydro-1, 2-naphthalenedicarboxylic anhydride with malonic acid in pyridine provided a convenient method for 2-acetyl-1-naph-thoic-or 2-acetyl-3, 4-dihydro-1-naphthoic acid. The structures of the products were also established.
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Takeo Ueda, Kiyoshi Takahashi, Sachiko Kobayashi
1964 Volume 12 Issue 4 Pages
497-499
Published: April 25, 1964
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Thermal reaction of equimolar amounts of 1, 1-(2, 2'-oxydiethyl) biguanide with dicyanodiamide afforded a compound (I) other than the both reactants. The analytical data, infrared spectra, and chemical properties of I agreeded closely with those of 2-morpho-lino-4, 6-diamino-s-triazine, synthesized by conventional manner from cyanuric chloride, ammonia, and morpholine. Consequently, I was verified to be 2-morpholino-4, 6-diamino-s-triazine.
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Teiichiro Ito
1964 Volume 12 Issue 4 Pages
499-501
Published: April 25, 1964
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On treating with trifluoroacetic acid, 2-benzyloxycarbonylamino-2-deoxy-1, 3, 4, 6-tetra-O-acetyl-β-D-glucopyranose afforded 2-amino-2-deoxy-1, 2-O, N-carbonyl-3, 4, 6-tri-O-acetyl-D-glucopyrane.
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Masamichi Tsuboi, Shigesada Higuchi, Yoshimasa Kyogoku, Kimiko Matsuo, ...
1964 Volume 12 Issue 4 Pages
501-503
Published: April 25, 1964
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Tadamasa Onaka, Susumu Kamata, Takashi Maeda, Yutaka Kawazoe, Mitsutak ...
1964 Volume 12 Issue 4 Pages
506-512
Published: April 25, 1964
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Yosisige Kato
1964 Volume 12 Issue 4 Pages
512-514
Published: April 25, 1964
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Yoshikazu Kondo, Kazue Kondo, Tsunematsu Takemoto, Tsuneo Ikenoue
1964 Volume 12 Issue 4 Pages
514-516
Published: April 25, 1964
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Minoru Goto, Shunji Imai, Tadakazu Murata, Shoji Fujioka
1964 Volume 12 Issue 4 Pages
516-518
Published: April 25, 1964
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Chiyoko Satoh, Akio Kiyomoto, Tomoharu Okuda
1964 Volume 12 Issue 4 Pages
518-520
Published: April 25, 1964
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