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Letters in Organic Chemistry


ISSN (Print): 1570-1786
ISSN (Online): 1875-6255

Research Article

A Novel Synthetic Approach to Diarylmethylpiperazine Drugs

Author(s): Tian Yu, Hongbo Dong*, Zheng Shi*, Lijia Cheng, Xiaoheng Guo, Xinjie Lian and Feng Liu

Volume 15 , Issue 6 , 2018

Page: [485 - 490] Pages: 6

DOI: 10.2174/1570178615666180110161450

Price: $65


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.

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