发明名称 Preparation of (R)-N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide and (S)-N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide
摘要 The present invention relates to the preparation of (R)—N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide and (S)—N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide.
申请公布号 US9296686(B2) 申请公布日期 2016.03.29
申请号 US201414467424 申请日期 2014.08.25
申请人 ARDEA BIOSCIENCES, INC. 发明人 Maderna Andreas;Vernier Jean Michel
分类号 C07C303/00;C07C303/38;C07C317/18;C07D317/26 主分类号 C07C303/00
代理机构 Millen White Zelano and Branigan, PC 代理人 Millen White Zelano and Branigan, PC ;Henter Csaba;Zelano Anthony
主权项 1. A process for preparing a compound of formula (I-a): comprising, contacting 5,6-difluoro-N1-(2-fluoro-4-iodophenyl)-3-methoxybenzene-1,2-diamine with a compound of formula (II-a): wherein R1 is H or an alcohol protecting group; R2 is H or an alcohol protecting group; or R1 and R2 together with the carbon atoms to which they are attached form a cyclic 1,2-diol protecting group.
地址 San Diego CA US