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Volume 13, Issue 11
Displaying 1-20 of 20 articles from this issue
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Yoshiyasu Furukawa, Kunio Kobayashi, Yoshio Kanai, Mikio Honjo1965 Volume 13 Issue 11 Pages 1273-1278
Published: November 25, 1965
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSMethylation of 3', 5'-di-O-trityluridine (I) gave a mixture of two compounds, which was detritylated and then separated to give N3, 2'-O-dimethyluridine (V) and 2'-O-methyluridine (VI). After treatment of the above mixture with ethanolic ammonia, the reaction products were detritylated and separated to give V and 2'-O-methyl-cytidine (VII). By a similar method 3'-O-methyl nucleosides were obtained from 2', 5'-di-O-trityluridine (II). The relative rates of acidic hydrolysis of uridine, VI, and 3'-O-methyluridine have been determined and were shown to obey first order kinetics. Introduction of a methoxyl function at the 2'- or 3'-position of uridine enhances the stability of the glycosyl linkage to acid hydrolysis.View full abstractDownload PDF (705K) -
Hideo Yamada, Ryuichi Yamamoto1965 Volume 13 Issue 11 Pages 1279-1284
Published: November 25, 1965
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS1) The model of absorption of drug in micellar solution from the intestine is proposed. According to this model, the relationship between concentration of the surfactant and absorption rate constant of the drug was derived. The calculated values of the absorption rate constants from the equation were compared with the experimentally observed values.2) The determination of absorption rate constant was carried out by the perfusion of salicylamide solutions containing polysorbate-80 in various concentrations through the rat small intestine in situ. 3) The experimental results indicate that there is a quite agreement between the observed value and the calculated value.View full abstractDownload PDF (692K) -
Takuichi Miki, Kentaro Hiraga, Tsunehiko Asako1965 Volume 13 Issue 11 Pages 1285-1289
Published: November 25, 1965
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA short step synthesis of estradiol was presented. 1-Vinyl-6-methoxy-1-tetralol (I) was condensed with 2-methyl-1, 3-cyclopentanedione (II)in the presence of Triton B to give dl-3-methoxy-8, 14-secoestra-1, 3, 5(10), 9-tetraene-14, 17-dione (III) which was converted by phosphorus pentoxide into the known dl-3-methoxyestra-1, 3, 5(10), 8, 14-pentaen-17-one(IV). The ketone (IV) was treated with sodium borohydride in methanol, yielding dl-3-methoxyestra-1, 3, 5(10), 8, 14-pentaen-17β-ol(V). Catalytic hydrogenation of this compound over Raney nickel was found to be stereospecific, yielding dl-3-methoxyestra-1, 3, 5, (10), 8-tetraen-17β-ol(VI). This compound was subjected to K-NH3reduction to give dl-estradiol 3-methyl ether (VII).Racemic V was resolved through its 17 l-menthoxyacetate and d-estradiol 3-methyl ether obtained by the above series of reactions was identical with the material of natural origin. dl-Equilenin 3-methyl ether was prepared from dl-3-methoxyestra-1, 3, 5(10), 8-tetraen-17β-ol (VI) by oxidation with Jones' reagent at one step.View full abstractDownload PDF (648K) -
Kentaro Hiraga1965 Volume 13 Issue 11 Pages 1289-1294
Published: November 25, 1965
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDuring the course of the synthesis of 18-methylestradiol 3-methyl ether, steric effect caused by the methyl group at 18-position was observed. It was found that ethylenediamine was a good solvent for the ethynylation reaction of the hindered ketone. Racemic and optically active 17β-hydroxy-13β, 17α-diethylgon-4-en-3-one were synthesized from 1-vinyl-6-methoxy-1-tetralol and 2-ethyl-1, 3-cyclopentanedion. The dextrorotatory diethylgonenone as well as the corresponding racemic diethylgonenone showed strong anabolic activities, whereas the levorotatory compound had no biological activity.View full abstractDownload PDF (719K) -
Kentaro Hiraga, Tsunehiko Asako, Takuichi Miki1965 Volume 13 Issue 11 Pages 1294-1299
Published: November 25, 1965
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSdl-18, 18-Dimethylestradiol 3-methyl ether (XII), dl-18, 18-dimethyl-19-nortestosterone (II) and their derivatives were synthesized starting from 1-vinyl-6-methoxy-1-tetralol (III) and 2-isopropyl-1, 3-crclopentanedione (IV). The steric effect of the 13-isopropyl group over 17-position was observed in every kind of reactions in this series. Both II and dl-17α-ethyl-18, 18-dimethyl-19-nortestosterone (XX) showed almost no anabolic and androgenic activity.View full abstractDownload PDF (752K) -
Kentaro Hiraga1965 Volume 13 Issue 11 Pages 1300-1306
Published: November 25, 1965
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSBased on the results of physicochemical measurements, the enolic forms of 1, 3-cyclopentanediones (IV), 1, 2, 4-cyclopentanetriones (XI), semicarbazones of 1, 2, 4-cyclopentanetriones and ethyl 2, 4, 5-trioxocyclopentylglyoxylate were discussed, and the structures (IX, XII, XV, and XVI) were proposed respectively.View full abstractDownload PDF (633K) -
Zen-ichi Horii, Masazumi Ikeda, Yasumitsu Tamura, Seiichi Saito, Keish ...1965 Volume 13 Issue 11 Pages 1307-1311
Published: November 25, 1965
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe leaves of Securinega suffruticosa REHD. furnished three new alkaloids, securinol A, B and C. The structures of securinol A and B were investigated.View full abstractDownload PDF (637K) -
Zen-ichi Horii, Yasuhiko Yamawaki, Yasumitsu Tamura, Seiichi Saito, Hi ...1965 Volume 13 Issue 11 Pages 1311-1318
Published: November 25, 1965
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDegradations of allosecurinine (III) gave the N-acetyl amino-lactone (IX), lactam-car-binol C (XIII), quinolizidine C (XVI), tetrahydroallosecurinine (XVIII) and compound (XIX). Identifications of the former three compounds (IX), (XIII) and (XVI) with the corresponding synthetic specimens provided a definite proof for the relative configuration of allose-curinine (III).View full abstractDownload PDF (948K) -
Minoru Sekiya, Yoshiro Osaki1965 Volume 13 Issue 11 Pages 1319-1325
Published: November 25, 1965
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFormation of 5-acetamido-substituted thiazoles was found to be readily effective on heating 2-(acylamino)thioacetamides with acetic anhydride. In additon, preparation of some starting 2-(acylamino)thioacetamides is described and 5-acetamidothiazole-4-carboxamides obtained by the thiazole formation reaction were led to some thiazolo[5, 4-d]pyrimidines.View full abstractDownload PDF (958K) -
Haruaki Yajima, Kazuo Kubo, Yoshio Okada1965 Volume 13 Issue 11 Pages 1326-1331
Published: November 25, 1965
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe syntheses of three pentapeptide isomers, L-histidyl-D-phenylalanyl-D-arginyl-L-tryptophylglycine (II), D-histidyl-D-phenylalanyl-D-arginyl-L-tryptophylglycine (III) and L-histidyl-D-phenylalanyl-D-arginyl-D-tryptophylglycine (IV) were described. Nα-Ben-zyloxycarbonyl-D-phenylalanyl-NG-nitro-D-arginine served as a key intermediate for the synthesis of these isomers. Melanocyte-stimulating activities of these compounds were examined using the frog-skin from Rana pipiens. It was found that II possessed the activity identical to that of L-histidyl-L-phenylalanyl-L-arginyl-L-tryptophylglycine (I). The peptides (III) and (IV) were both inactive.View full abstractDownload PDF (846K) -
Hiroshi Mitsuhashi, Taro Nomura1965 Volume 13 Issue 11 Pages 1332-1340
Published: November 25, 1965
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe structure of benzoylramanone (III), a new ester type aglycone from Metaplexis japonica MAKINO, has been proved by chemical conversions and spectroscopic examination of the conversion products. The structural conclusion have been confirmed by correlation with a degradation product from hecogenin.View full abstractDownload PDF (998K) -
Masao Tomita, Kazuyoshi Fujitani, Yoshiaki Aoyagi1965 Volume 13 Issue 11 Pages 1341-1345
Published: November 25, 1965
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSCupric oxide catalyst improved the yield in some Ullmann condensation reactions affording diaryl ether derivatives. Though it was not concluded whether cupric oxide was the ture catalytic species or not, its efficiency was proved.View full abstractDownload PDF (610K) -
Takao Murakami, Hideji Itokawa, Fumiko Uzuki, Naotoshi Sawada1965 Volume 13 Issue 11 Pages 1346-1352
Published: November 25, 1965
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIt was discussed that the relations between Rf values and the structures of 50 samples of triterpenoids and related compounds on silica gel G and alumina G, using 11 kinds of solvent systems. Four konds of reagents were used for detection.View full abstractDownload PDF (641K) -
Mitsuya Tanaka, Yoshiko Toshimitsu1965 Volume 13 Issue 11 Pages 1353-1358
Published: November 25, 1965
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSMethyl N-(benzyloxycarbonylaminoacyl)-β-D-glucosaminides and N-(benzyloxycarbonylaminoacyl)-D-glucosaminols were prepared and the periodate oxidation of some of these compounds was studied. Saponification of N-(β-benzyl-N-benzyloxycarbonyl-α-L-aspartyl)-tri-O-acetyl-D-glucosaminide (IIId) caused a transpeptidation to give the β-aspartyl derivative (IVd) and the α-isomer (IVf) was prepared by deacetylation of N-(N-benzyloxycarbonyl-α-aspartyl)-tri-O-acetyl-D-glucosaminide (IIIf), which was obtained by the reaction of N-benzyloxycarbonyl-L-aspartic anhydride with methyl-tri-O-acetyl-β-D-glucosaminide (II).View full abstractDownload PDF (817K) -
Kentaro Hiraga1965 Volume 13 Issue 11 Pages 1359-1361
Published: November 25, 1965
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS2-Ethyl, 2-isopropyl and 2-benzyl-1, 3-cyclopentanediones were synthesized by the known method. Diethyl 2-methyl-3-oxoadipate was cyclized to 2-methyl-1, 3-cyclopentanedione by heating with potassium tert-butoxide. 3-Methyl-1, 2, 4-cyclopentanetrione was reduced to 2-methyl-1, 3-cyclopentanedione by Clemmensen method.View full abstractDownload PDF (394K) -
Mahmoud M. El-Merzabani1965 Volume 13 Issue 11 Pages 1362-1363
Published: November 25, 1965
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA simple method was described for the synthesis of 3, 3'-dimesyloxy-N-methyl[14C]-dipropylamine hydrochloride in 29% yield, together with a method for recovery of the aminoalcohol (II) from the impure dimesyloxy derivative.View full abstractDownload PDF (365K) -
Yoshio Sakurai, Mahmoud M. El-Merzabani1965 Volume 13 Issue 11 Pages 1363-1365
Published: November 25, 1965
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSix new derivatives of sulfonic acid esters of aminoglycols were prepared and tested for their carcinostatic activity against Yoshida sarcoma. All the tested compounds showed strong cytomorphological effects on the tumor cells but not effective in prologation of life span of the tumor bearing animals.View full abstractDownload PDF (450K) -
Yoshio Arata, Tsutomu Ohashi1965 Volume 13 Issue 11 Pages 1365-1368
Published: November 25, 1965
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSJudging from the nuclear magnetic resonance spectra of I, IV and VI, the formula (VII) would be presented as the absolute configuration of nuphamine.View full abstractDownload PDF (413K) -
Seiji Miyano, Yoko Sako1965 Volume 13 Issue 11 Pages 1372-1373
Published: November 25, 1965
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDownload PDF (343K) -
Fumio Kai, Shigeo Seki1965 Volume 13 Issue 11 Pages 1374-1376
Published: November 25, 1965
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDownload PDF (446K)
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