发明名称 Process for the preparation of 3-aroyl-5-aminobenzofuran derivatives
摘要 The present invention relates to a process for the preparation of 3-aroyl-5-aminobenzofuran derivatives useful as antiarrhythmic drugs which avoids the use of nitro intermediates.
申请公布号 US9512097(B2) 申请公布日期 2016.12.06
申请号 US201113884179 申请日期 2011.11.11
申请人 Lek Pharmaceuticals D.D. 发明人 Richter Frank;Schreiner Erwin;Pirc Samo;Copar Anton
分类号 C07D307/00;C07D307/81;C07D307/82;C07D307/84;A61K31/343 主分类号 C07D307/00
代理机构 Arent Fox LLP 代理人 Arent Fox LLP
主权项 1. A process for the preparation of a compound of Formula V or a salt thereof wherein R1 is selected from C1-C8-alkyl, R2 is selected from the group consisting of: C1-C8-alkyl, fluorinated C1-C8-alkyl, phenyl, and para substituted phenyl, and Z is cyano or C(O)R, wherein R represents a benzene ring having a halo substituent in none, one or both of the meta positions and having a fluoro, chloro, bromo, iodo, nitro, C1-C8-alkyl, substituted C1-C8-alkyl, hydroxy, C1-C8-alkoxy, substituted C1-C8-alkoxy, C1-C8-alkylamino, or substituted C1-C8-alkylamino substituent in para position, the process comprising a) treating a sulfonimidoquinone of Formula III with a compound of Formula IV in enolic or ketonic tautomeric form, wherein Y is selected from the group consisting of: hydroxy, C1-C2-alkoxy, phenoxy, —OSi(Ra)3 wherein Ra is the same or different and selected from the group consisting of: C1-C4-alkyl and phenyl, —OSO2Rb wherein Rb is unsubstituted or fluorinated C1-C4-alkyl, or phenyl, and —OP(O)(ORc)2 wherein Rc is selected from the group consisting of: C1-C4-alkyl, and phenyl, and Z is as defined above.
地址 Ljubljana SI