Potential Antiinflammatory Agents. V. Synthesis of Metabolites of 6-Chloro-5-cyclohexylindan-1-carboxylic Acid (TAI-284) using Microbiological Hydroxylation
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概要
- 論文の詳細を見る
Microbiological hydroxylation of 6-chloro-5-cyclohexylindan-1-carboxylic acid (TAI-284), a new potent antiinflammatory agent, with Penicillium concavo-rugulosum IFO 6226 gave 6-chloro-5-(trans-4'-hydroxycyclohexyl) indan-1-carboxylic acid (1), one of the main metabolites of TAI-284 in rats, in 71% yield. From this product two other metabolites, the corresponding 4'-oxo and cis-4'-hydroxy derivatives (4 and 2), were derived chemically. Catalytic hydrogenation of the 4'-oxo compound (4) over PtO_2 afforded the unexpected trans alcohol (1), but reduction of 4 with trimethylphosphite and iridium tetrachloride in aqueous isopropanol gave the desired cis alcohol (2) in 69% yield.
- 社団法人日本薬学会の論文
- 1976-04-25
著者
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岸本 彰二
Pharmaceutical Research Laboratories Iii Takeda Chemical Industries Ltd.
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岸本 彰二
Central Research Division, Takeda Chemical Industries, Ltd.
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野口 俊作
Central Research Division, Takeda Chemical Industries, Ltd.
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杉野 弘
Central Research Division, Takeda Chemical Industries, Ltd.
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田中 邦大
Central Research Division, Takeda Chemical Industries, Ltd.
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垣沼 淳司
Central Research Division, Takeda Chemical Industries, Ltd.
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野口 俊作
Central Research Division Takeda Chemical Industries Ltd.
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岸本 彰二
Pharmaceutical Research Laboratories Iii Pharmaceutical Research Division Takeda Chemical Industries
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田中 邦大
Central Research Division Takeda Chemical Industries Ltd.
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