发明名称 Preparation of (r)- and (s)-n-(3, 4-difluoro-2-(2-fluoro-4-iodophenylamino)--6-methoxyphenyl) -1- (2, 3-dihydroxypropyl)cyclopropane-1-sulfonamide and protected derivatives thereof
摘要 597738 Disclosed herein is a process for preparing (R)- and (S)-N-(3,4-Difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide comprising: i) contacting 5,6-difluoro-N1-(2-fluoro-4-iodophenyl)-3-methoxybenzene-1,2-diamine with a sulfonyl chloride of formula (II-a) or formula (II-b); and ii) contacting a protected diol of formula (I-a) or formula (I-b) with an acid, a base or a nucleophile, or exposing the compound of formula (I-a) or formula (I-b) to UV light. Additionally disclosed are intermediate compounds Additionally disclosed are intermediate compounds (R)- and (S)-1-((2,2-dimethyl-1,3-dioxolan-4-yl)methyl)cyclopropane-1-sulfonyl chloride, and (R)- and (S)-3-(2,2-dimethyl-1,3-dioxolan-4-yl)prop-1-ene-2-sulfonyl chloride.
申请公布号 NZ597738(A) 申请公布日期 2014.03.28
申请号 NZ20100597738 申请日期 2010.07.10
申请人 ARDEA BIOSCIENCES INC. 发明人 VERNIER JEAN-MICHEL;MADERNA ANDREAS
分类号 C07C303/38;C07C303/40;C07C309/82;C07C309/85;C07C311/28 主分类号 C07C303/38
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