Synthetic Studies on Psychotropic Agents. I. A New Synthesis of 2'-Amino-4'-fluorobutyrophenone Derivatives using a Serective ortho-Amination of 2', 4'-Difluorobutyrophenone Derivatives

Abstract

A new synthesis of 2'-amino-4'-fluoro-4-[4-hydroxy-4-(α, α, α-trifluoro-m-tolyl) piperidino] butyrophenone using a selective ortho-amination as a key step was described. The solvents and temperature effects on the selectivity for this ortho-amination of 2', 4'-difluoro-4-[4-hydroxy-4-(α, α, α-trifluoro-m-tolyl) piperidino] butyrophenone were investigated.