发明名称 Method for preparing 3-keto-benzofurane derivatives
摘要 The invention relates to a method for preparing 3-keto-benzofurane derivatives of the general formula: Formula (I), where R is an alkyl or aryl group, R1 is hydrogen or an alkyl or aryl group, and R2 is a substituted alkyl or phenyl group. Said preparation method involves coupling a derivative of Formula III, where X is chlorine, bromine, or iodine or a sulfonate grouping: Formula (III) with a sulfonamide derivative of the formula R—SO2—NH2 in the presence of a basic agent and a catalytic system formed of a complex between a palladium compound and a ligand.
申请公布号 US8871956(B2) 申请公布日期 2014.10.28
申请号 US201113638484 申请日期 2011.03.30
申请人 Sanofi 发明人 Bailly Fréderic;Priem Thomas;Vayron Philippe
分类号 C07D307/00;C07D307/81;C07D307/80;C07D307/79 主分类号 C07D307/00
代理机构 Scully, Scott, Murphy & Presser, P.C. 代理人 Scully, Scott, Murphy & Presser, P.C.
主权项 1. A method for preparing 3-keto-benzofuran derivatives of general formula: in which R represents an alkyl or aryl group, R1 represents hydrogen or an alkyl or aryl group and R2 represents an alkyl or phenyl group of general formula: in which Y represents hydrogen, a halogen or a hydroxyl, alkoxy or dialkylaminoalkoxy group, where a benzofuran derivative of general formula: in which R1 and R2 have the same meanings as above and X represents chlorine, bromine or iodine or a sulfonate group of general formula: R3—SO2—O—  IV in which R3 represents a trifluoromethane or imidazolyl group; is coupled with a sulfonamide derivative of general formula: R—SO2—NH2  V in which R has the same meaning as above, in the presence of a basic agent and a catalytic system formed of a complex between a palladium compound and a ligand.
地址 Paris FR