Patent ID: 7126009

Claim:
A method for making substituted indole compounds comprising the steps of: reacting a 2-bromoaniline or 2-chloroaniline of formula (I) wherein: X is Br or Cl, R is H, alkyl, aryl, —C(O)C 1-6 alkyl, —C(O)-aryl, —S(O) 2 C 1-6 alkyl or —S(O) 2 aryl; R 1 is C 1-6 alkyl, C 1-6 alkoxy, —CO 2 C 1-6 alkyl, C 1-6 alkylHNC(O)—, and with a substituted acetylene of formula (II) wherein R 2 is acyclic or cyclic alkyl, aryl, or heterocycly; R 3 is: phenyl optionally substituted with F, Cl, alkyl, aryl, CO 2 C 1-6 alkyl or carboxamide, or R 3 is heteroaryl selected from pyridine, pyrimidine, furan, thiophene, pyrrole and imidazole, optionally substituted with F, Cl, alkyl, aryl, CO 2 C 1-6 alkyl or carboxamide, or R 3 is trialkysilyl, alkyl, alkoxy; in the presence of a palladium catalyst, a ligand, and a base in a solvent to give a compound of formula (III);