Abstract

Classical methods for the synthesis of diarylmethylpiperazine drugs generally lead to the generation of high levels of waste. In this study, we have developed a simple and efficient route to the anti-histamine drugs Meclizine 1, Buclizine 2, Clocinizine 3, Cinnarizine 4, Flunarizine 5 and Flotrenizine 6. The advantage of this route lies on the replacement of harmful alkyl halides by readily available alcohols to achieve the N-alkylation of the piperazine unit. This procedure was further extended to the synthesis of other diarylmethylpiperazine drugs and derivatives.

Keywords: Diarylmethylpiperazine drugs, N-alkylation, synthesis, anti-histamine drugs, derivatives, alcohol.

Graphical Abstract