Process for preparing 2,3-disubstituted indoles

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 C 1-5 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.