A novel synthetic approach to very late antigen-4 antagonist trans-4-〔1-〔〔2,5-dichloro-4-(1-methyl-3-indolylcarboxyamide)phenyl〕acetyl〕-(4S)-methoxy-(2S)-pyrrolidinylmethoxy〕cyclohexanecarboxylic acid via tert-butyl trans-〔(4S)-methoxy-(2S)-pyrrolidinylmethoxy〕cyclohexanecarboxylate as a key intermediate

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  • Chiba Jun
    Lead Discovery & Optimization Research Laboratories II, Daiichi Sankyo Co., Ltd.
  • Machinaga Nobuo
    Lead Discovery & Optimization Research Laboratories II, Daiichi Sankyo Co., Ltd.

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  • A Novel Synthetic Approach to Very Late Antigen-4 Antagonist trans-4-[1-[[2,5-Dichloro-4-(1-methyl-3-indolylcarboxyamide)phenyl]acetyl]-(4S)-methoxy-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylic Acid via tert-Butyl trans-[(4S)-Methoxy-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylate as a Key Intermediate

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This contribution describes a novel synthetic approach to very late antigen-4 (VLA-4) antagonist trans-4-[1-[[2,5-dichloro-4-(1-methyl-3-indolylcarboxyamide)phenyl]acetyl]-(4S)-methoxy-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylic acid (1) via tert-butyl trans-[(4S)-methoxy-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylate (2b) as a key intermediate. The synthesis, which includes n-Bu4NSO3H that catalyzed basic etherification of 12 and iodine-mediated cyclization to provide the 2,4-disubstituted pyrrolidine frame of 2b, is designed to utilize trans-4-hydroxycyclohexanecarboxylic acid (9) as a commercially available starting material.

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