abstract |
A process for making a substituted indole derivative of formula (I) is disclosed, wherein said process comprises: reacting a substituted indole compound of formula (I') with a heteroaryl or aryl zinc halide or di-heteroaryl or di-aryl zinc compound as defined in the specification, wherein the variables are as defined in the specification, and wherein the reaction is carried out in the presence of a metal catalyst selected from Pd and Ni, a ligand selected from mono-dentate triphenylphosphine (Ph3P), tri-p-tolylphosphine (p-Tol3P), tricyclohexylphosphine (PCy3), tri-t-butylphosphine (t-Bu3P), (Cy2P(Ph-Ph)) and bi-dentate 1,1'-bis(diphenylphosphino)ferrocene (dppf), 1,4-bis(diphenylphosphino)ferrocene (dppb), in a solvent selected from tetrahydrofuran (THF), dimethoxyethane (DME), dimethylformamide (DMF), 1-methyl-2-pyrrolidinone (NMP) or a combination thereof, at a temperature of between ambient and 100 Deg. C, to provide the desired compound of formula (I). |