Expedient Preparations of 2-Trifluoromethylindole and Its N-Methyl Derivative

Abstract

Procedures have been developed which provide direct regiocontrolled syntheses of 2-trifluoromethylindole and l-methyl-2trifluoromethylindole from readily available starting materials in moderate yields.Heterocyclic compounds containing trifluoromethyl substituents have important 1 applications in medicinal and agricultural chemistry.Despite the variety of trifluoromethylated heterocycles that are available, references in the literature for Z-trifluoromethylindole or its derivatives are sparse, presumably due to the lack of reasonable approaches to these ~o m ~o u n d s .~-~In this paper we describe practical methods for the preparation of the parent 2-trifluoromethylindole and its N-methylated derivative, Three syntheses of 2-trifluoromethylindole have been reported.One of these methods