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TAISUKE ITAYA, CHIEKO SHIOYAMA, SEIYA KAGATANI
1982Volume 30Issue 9 Pages
3392-3394
Published: September 25, 1982
Released on J-STAGE: March 31, 2008
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An improved procedure for the synthesis of 3-methylguanine (4) from 2, 6-diamino-1-methyl-4-pyrimidone (1) is presented. Elemental analyses and ultraviolet (UV) and nuclear magnetic resonance (NMR) spectral data are presented for the compounds involved in the reaction sequence.
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YOSHIAKI WAKITA, TOSHIO KOBAYASHI, MINORU MAEDA, MASAHARU KOJIMA
1982Volume 30Issue 9 Pages
3395-3398
Published: September 25, 1982
Released on J-STAGE: March 31, 2008
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Lithium N-methylanilide, prepared from N-methylaniline and n-butyllithium, readily absorbed CO at atmospheric pressure in the presence of cuprous iodide to produce a CO-containing copper complex. Treatment of this complex with organic halides gave the corresponding amides in good yields.
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YASUSHI TAKEDA, HIROKO KANAYA
1982Volume 30Issue 9 Pages
3399-3404
Published: September 25, 1982
Released on J-STAGE: March 31, 2008
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A general procedure for screening for the formation of nitroso derivatives and/or mutagens by drug-nitrite interaction was established. A test drug (50 mM) was reacted with nitrite (500 mM) at pH 3.0-3.5 and 37°C for 4 h. The residual nitrite in the reaction mixture was decomposed with ammonium sulfamate. The nitrite-free reaction mixture was assayed for both nitroso derivatives and mutagens by colorimetry of Griess reagentpositive substances formed by treatment with hydrogen bromide and by mutagenesis assay using Salmonella typhimurium TA98 and TA100 as tester strains, respectively.
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SHOZO MIYAZAKI, KUNIAKI ISHII, MASAHIKO TAKADA
1982Volume 30Issue 9 Pages
3405-3407
Published: September 25, 1982
Released on J-STAGE: March 31, 2008
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Fibrin film was evaluated as a new carrier for a long-acting delivery system for pilocarpine. The release characteristics of the pilocarpine-fibrin film system were investigated in in vitro and in vivo test models. The results indicated that the use of the pilocarpinefibrin film system is more effective than that of the conventional liquid dosage form for prolonging the duration of a desirable pupillary response. Its good biocompatibility, flexibility, and heat processability suggest the material to be a good candidate system for pilocarpine delivery into the eye.
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MASAHIKO TAKADA, SHOZO MIYAZAKI, KAZUMOTO CHIBA, MIEKO SAKAMOTO, MEGUM ...
1982Volume 30Issue 9 Pages
3408-3413
Published: September 25, 1982
Released on J-STAGE: March 31, 2008
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An interaction study between sulfonamides and non-steroidal anti-inflammatory agents similar to that described in the previous paper was repeated in dogs to confirm the previous findings and conclusions. Pharmacokinetic parameters were calculated from the plasma levels after intravenous administration using a two-compartment open model. The data are presented and compared with those given in previous reports.
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Masao Wada, Hideo Nakai, Yasuhiko Sato, Yuichi Kanaoka
1982Volume 30Issue 9 Pages
3414-3417
Published: September 25, 1982
Released on J-STAGE: March 31, 2008
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Based on a regioselective remote photocyclization of a pair system consisting of a phthalimide group and a dithiolanyl group, a variety of aza-cyclic compounds with methylene, ester, or amide groups in their frameworks were synthesized. The dithiolanyl group provides a removable donor, which effects a subsequent reaction followed by removal to give a new carbon skeleton.
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Shunsuke Naruto, Norio Nagamoto, Hiroyuki Mizuta, Toyokichi Yoshida, H ...
1982Volume 30Issue 9 Pages
3418-3420
Published: September 25, 1982
Released on J-STAGE: March 31, 2008
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Reactions of 1, 2-benzisoxazole-3-acetic acid (1) with tosyl chloride and acyl chlorides in pyridine afforded the corresponding 4-oxo-4H-benzisoxazolo [2, 3-a] pyridines (2).
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Shunsuke Naruto, Norio Nagamoto, Hiroyuki Mizuta, Toyokichi Yoshida, H ...
1982Volume 30Issue 9 Pages
3421-3423
Published: September 25, 1982
Released on J-STAGE: March 31, 2008
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Photolysis of 4-oxo-4H-benzisoxazolo [2, 3-a] pyridines (1a-d) and their C
1-monobromides (4a-d) afforded benzofuro [3, 2-b] pyridines (2a-d) via initial N
5-O
6 bond fission. However, similar photolysis of 9-methoxy-4-oxo-4H-benzisoxazolo [2, 3-a] pyridine analog (4f) gave a pyridine derivative (5).
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Taisei Ueda, Yoshitsugu Shibata, Jinsaku Sakakibara, Masatoshi Inoue, ...
1982Volume 30Issue 9 Pages
3424-3426
Published: September 25, 1982
Released on J-STAGE: March 31, 2008
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The reaction of 5-amino-6-methyl-3-phenyl-4 (3H)-pyrimidone (1) with selenium dioxide in dioxane gave the unusual products : 6-phenyl-7 (6H)-isoselenazolo [4, 3-d] pyrimidone (2) and 3-phenylcarbamoyl-4-methyl-1, 2, 5-selenadiazole (3) in the ratio 1 : 2.
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Norio Aimi, Sohei Tanabe, Yoshihisa Asada, Yoko Watanabe, Keiichi Yama ...
1982Volume 30Issue 9 Pages
3427-3430
Published: September 25, 1982
Released on J-STAGE: March 31, 2008
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A smooth skeletal rearrangement took place when a chloroindolenine (2) derived from 3-oxotabersonine (1) was treated under solvolytic conditions. The structure of the rearrangement product (3) was clarified unambiguously by X-ray crystal analysis.
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Motomasa Kobayashi, Tohru Yasuzawa, Yoshimasa Kyogoku, Masaru Kido, Is ...
1982Volume 30Issue 9 Pages
3431-3434
Published: September 25, 1982
Released on J-STAGE: March 31, 2008
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Three new sesquiterpenes named valerenenol (1), isovalerenenol (2), and anhydrovalerenenol (3), having a new carbon skeleton of ent-valere-nane, were isolated from an Okinawan soft coral (unidentified sp., Xeniidae) and their absolute stereostructures were elucidated by chemical, physicochemical, and X-ray crystallographic analyses.
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Kiyoshi Tatsumi, Yoshihiro Takahashi
1982Volume 30Issue 9 Pages
3435-3438
Published: September 25, 1982
Released on J-STAGE: March 31, 2008
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The metabolic fate of the widely used veterinary drug, furazolidone (N-(5-nitro-2-furfurylidene)-3-amino-2-oxazolidone) was examined in rats. When
14C-furazolidone was administered orally to rats, most of the radioactivity was recovered from urine and feces during the first 24 hr, indicating rapid clearance of the nitrofuran from the animal bodies. The radioactivity in feces appears to be partly due to its biliary excretion and partly due to its exsorption. Two metabolites of the nitrofuran were isolated from the urine and unequivocally identified as 3-(4-cyano-2-oxobutylideneamino)-2-oxazolidone and N-(5-acetamido-2-furfurylidene)-3-amino-2-oxazolidone by comparison with authentic specimens.
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Shoji Okada, Mizue Suzuki, Hideo Tsukada, Hiroshi Ohba
1982Volume 30Issue 9 Pages
3439-3441
Published: September 25, 1982
Released on J-STAGE: March 31, 2008
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The administration of trivalent chromium (Cr (III)) caused a significant enhancement of RNA synthesis in rat liver after partial hepatectomy. Cr was accumulated in the liver cell nuclei and concentrated in the nucleoli. Of RNAs synthesized in the nuclei, nucleolar RNA synthesis was most enhanced by the administration of Cr (III). Furthermore, DNA synthesis in the Cr (III)-administered rat liver after partial hepatectomy was initiated a little earlier and was less synchronized than in control rats.
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Mitsutaka Natsume, Masashi Ogawa
1982Volume 30Issue 9 Pages
3442-3445
Published: September 25, 1982
Released on J-STAGE: March 31, 2008
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The 1-acyl-2, 6-cis-disubstituted 1, 2, 3, 6-tetrahydropyridine derivatives (5a-5d) were found to possess the structure of 5-A as a stable conformer. This knowledge was applied to a stereo-controlled formation of the side chain of palustrine (1) by causing an aldehyde (8) to react with Et
2CuLi. A chelated intermediate (8-C) may play an important role in the preferential production of the desired compound (9).
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Miyoji Hanaoka, Shunichiro Sakurai, Takeshi Ohshima, Shingo Yasuda, Ch ...
1982Volume 30Issue 9 Pages
3446-3449
Published: September 25, 1982
Released on J-STAGE: March 31, 2008
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Reduction of the 8, 14-cycloberbin-13-one (7a), derived from coptisine (6a), with LiAlH (OBu
t)
3 gave stereoselectively the alcohol (8a) which was subsequently treated with ethyl chloroformate to afford the oxazolidinone (10a). Hydrolysis of 10a followed by methylation with methyl iodide provided (±)-ochrobirine (1a).
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Toyohiko Aoyama, Takayuki Shioiri
1982Volume 30Issue 9 Pages
3450-3452
Published: September 25, 1982
Released on J-STAGE: March 31, 2008
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Lithium trimethylsilyldiazomethane, prepared from trimethylsilyldiazomethane and lithium diisopropylamide, reacts smoothly with methyl esters of carboxylic acids to give 2-substituted 5-trimethylsilyltetrazoles in good yields.
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Masato Shimizu, Masayuki Ishikawa, Yasuo Komoda, Terumi Nakajima, Keii ...
1982Volume 30Issue 9 Pages
3453-3456
Published: September 25, 1982
Released on J-STAGE: March 31, 2008
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(1S)-(-)-Trypargine (1a) was synthesized from (1S, 3R)-(-)-2-benzyl-3-(methoxycarbonyl)-1, 2, 3, 4-tetrahydro-9H-pyrido [3, 4-b] indole-1-propionic acid (3a), prepared by the asymmetric Pictet-Spengler reaction of N
b-benzyl-(D)-tryptophan methyl ester (2) with α-ketoglutaric acid. The absolute configuration of natural trypargine (1a) at the C
1 position was determined to be the S-configuration.
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Yasuyuki Endo, Koichi Shudo, Toshihiko Okamoto
1982Volume 30Issue 9 Pages
3457-3460
Published: September 25, 1982
Released on J-STAGE: March 31, 2008
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A synthesis of 3, 4, 5, 6, 7, 8-hexahydro-6-oxo [1, 4] diazonino [7, 6, 5-cd] indoles (3 and 18) which have active fragments of teleocidins (1) and lyngbyatoxin (2) is described.
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