Chinese Journal of Organic Chemistry >
Synthesis of Antihistamine Drug Hydroxyzine with New N-Alkylation Method
Received date: 2016-04-29
Revised date: 2016-05-26
Online published: 2016-07-07
Supported by
Project supported by the Open Foundation of Antibioticis Research and Re-evaluation Key Laboratory of Sichuan Province (No.ARRLKF14-09).
The Raney-Ni catalyzed N-alkylation for the synthesis of antihistamine drug hydroxyzine (1a) has been developed. The substrate scope was expanded with the optimized reaction conditions, and fourteen diphenylmethyl piperazine derivatives including antihistamine drugs decloxizine (1j), mecilizine (1l), buclizine (1m) and calcium channel blocker lomerizine (1n) were successfully prepared. This Raney-Ni catalyzed N-alkylation was the first protocol that applied in these drugs synthesis. And this research improve its application value in drug synthesis.
Key words： hydroxyzine; drug synthesis; Raney-Ni; N-alkylation
Dong Hongbo , Zheng Dengyu , Luo Hongbing , Du Weihong , Lin Jiafu , Cao Shenghua . Synthesis of Antihistamine Drug Hydroxyzine with New N-Alkylation Method[J]. Chinese Journal of Organic Chemistry, 2016 , 36(11) : 2709 -2714 . DOI: 10.6023/cjoc201604060
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