发明名称 Process for preparing sulfonamidobenzofuran derivatives
摘要 The invention relates to a process for preparing 5-sulfonamido-benzofuran derivatives of general formula: formula (I) in which R represents an alkyl or aryl group and R1 and R2 represent hydrogen or an alkyl or aryl group. According to the invention, the compounds of formula I are prepared by coupling a benzofuran derivative of general formula II, where X represents chlorine, bromine or iodine or a sulfonate group: formula (II) with a sulfonamide derivative of formula R—SO2—NH2, in the presence of a basic agent and of a catalyst system formed from a complex between a palladium compound and a ligand.;
申请公布号 US9334254(B2) 申请公布日期 2016.05.10
申请号 US201113638500 申请日期 2011.03.30
申请人 SANOFI 发明人 Priem Thomas;Vayron Philippe Paul
分类号 C07D307/00;C07D307/79 主分类号 C07D307/00
代理机构 Morrison & Foerster LLP 代理人 Morrison & Foerster LLP
主权项 1. A process for preparing 5-sulfonamidobenzofuran derivatives of general formula: in which R represents an alkyl or aryl group and R1 and R2, which may be identical or different, each represent hydrogen or an alkyl or aryl group, comprising coupling a benzofuran derivative of general formula: in which R1 and R2 have the same meaning as previously and X represents chlorine, bromine or iodine or a sulfonate group of general formula: R3—SO2—O—   III in which R3 represents a trifluoromethane or imidazolyl group, with a sulfonamide derivative of general formula: R—SO2—NH2   IV in which R has the same meaning as previously, in the presence of a basic agent and of a catalytic system formed from a complex between a palladium compound and a ligand wherein the palladium compound is selected from the group consisting of bis(dibenzylideneacetone)palladium(0) and tris(dibenzylideneacetone)dipalladium (0), and wherein the ligand is 2-(di-tert-butylphosphino)-2′,4′,6′-triisopropyl-1,1′-biphenyl.
地址 Paris FR