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 |