Psychotropic Agents. VI. An Improved Synthetic Method for 4'-Fluoro-4-[4-(2-thioxo-1-benzimidazolinyl) piperidino] butyrophenone
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概要
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The title compound (8) was prepared by two improved methods. Initially, the 4-aminopiperidine derivative (11) was prepared by treatment of 4-aminopyridine (9) with the aralkyl chloride (5), followed by NaBH_4 reduction of the resulting 4-aminopyridinium salt (10). Reaction of 11 with 2-chloronitrobenzene gave the intermediate (6). Subsequently, the key intermediate (7) was similarly prepared starting from 4-chloropyridine (12) via the pyridinium salt (14). In this method the target compound (8) was prepared in good yield with the technical advantage that the four steps (13→14→7→8) could be conveniently carried out in a one-pot procedure.
- 公益社団法人日本薬学会の論文
- 1982-02-25
著者
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佐藤 誠
Faculty of Pharmaceutical Sciences Toyama Medical and Pharmaceutical University
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佐藤 誠
Research Institute, Daiichi Seiyaku Co., Ltd.,
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有本 昌弘
Research Institute, Daiichi Seiyaku Co., Ltd.
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有本 昌弘
Research Institute Daiichi Seiyaku Co. Ltd.
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