Process Development of Micafungin, a Novel Lipopeptide Antifungal Agent

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  • リポペプチド系抗真菌剤ミカファンギンの工業化
  • リポペプチドケイ コウシンキンザイ ミカファンギン ノ コウギョウカ

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The manufacturing process of Micafungin (1) which is a novel candin antifungal agent discovered and developed by Astellas Pharma Inc. was studied.<BR>A new asymmetric isoxazole ring formation which is key reaction for synthesis of side chain active ester 2 was developed via β-keto enamine intermediate.<BR>And also a reaction condition of selective acylation with FUN intermediate 3 and purification of Micafungin drug substance was investigated from the viewpoints of high quality and productivity.

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