利用新型氮烷基化方法合成抗组胺药物羟嗪
收稿日期: 2016-04-29
修回日期: 2016-05-26
网络出版日期: 2016-07-07
基金资助
抗生素研究与再评价四川省重点实验室开放基金（No.ARRLKF14-09）资助项目.
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).
董宏波 , 郑登宇 , 罗红兵 , 杜伟宏 , 林家富 , 曹胜华 . 利用新型氮烷基化方法合成抗组胺药物羟嗪[J]. 有机化学, 2016 , 36(11) : 2709 -2714 . DOI: 10.6023/cjoc201604060
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
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