公开(公告)号：EP1853589A1

公开(公告)日：2007-11-14

申请号：EP06734761.7

申请日：2006-02-10

申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH ,  Boehringer Ingelheim Pharma GmbH & Co. KG

发明人： KHODABOCUS, Ahmad ,  LU, Zhi-Hui ,  SENANAYAKE, Chris, H. ,  WEI, Hanxun ,  ZHANG, Yongda

IPC分类号： C07D403/04 ,  C07D409/04 ,  C07D401/04 ,  C07D209/08 ,  C07D209/12 ,  C07D209/10

CPC分类号： C07D209/10 ,  C07D209/08 ,  C07D209/12 ,  C07D401/04 ,  C07D403/04 ,  C07D409/04

摘要： Disclosed are processes for making 2, 3 disubstituted indole compounds such as compounds of general formula I comprised of the steps of a) reacting a bromoindole compound (i) with a dialkoxyl C1-5 borane in the presence of a ligand, a palladium catalyst and a base to make a compound of general formula (ii); or alternatively reacting compound (i) with a trialkyl magnesiate reagent, followed by treatment with a borate; b) reacting the product of step a with a R2-Hal where R2-Hal is defined herein.