Palladium catalyzed indolization of 2-bromo or chloroanilines
The present invention provides a method for making substituted indole compounds of general formula III comprising the step of:(a) reacting a 2-bromoaniline or 2-chloroaniline of general formula (I)(I)wherein: X, R and R1 are defined hereinwith a substituted acetylene of formula (II)wherein R2 and R3 are defined herein in the presence of a palladium catalyst, a ligand, and a base in a solvent at a suitable temperature to give a compound of formula (III);
Boehringer Ingelheim International, GmbH
C C C C
C07D C07C C07C C07D
inventional additional inventional inventional
Guisheng Jianxiu Zhi-Hui Chris Hugh Frank Ming
Li Liu Lu Senanayake Roschangar Shen