Synthesis of Antihistamine Drug Hydroxyzine with New N-Alkylation Method

doi:10.6023/cjoc201604060

Chin. J. Org. Chem. ›› 2016, Vol. 36 ›› Issue (11): 2709-2714.DOI: 10.6023/cjoc201604060 Previous Articles Next Articles

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利用新型氮烷基化方法合成抗组胺药物羟嗪

董宏波^a, 郑登宇^a, 罗红兵^a, 杜伟宏^a, 林家富^b, 曹胜华^a

a 成都大学四川抗菌素工业研究所药食同源植物资源开发四川省高校重点实验室成都 610052;
b 成都大学四川抗菌素工业研究所抗生素研究与再评价四川省重点实验室成都 610052

收稿日期:2016-04-29 修回日期:2016-05-26 发布日期:2016-07-07
通讯作者: 董宏波 E-mail:bloodwhenseeme@163.com
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

Dong Hongbo^a, Zheng Dengyu^a, Luo Hongbing^a, Du Weihong^a, Lin Jiafu^b, Cao Shenghua^a

a Key Laboratory of Medicinal and Edible Plants Resources Development of Sichuan Education Department, Sichuan Industrial Institute of Antibiotics, Chengdu University, Chengdu 610052;
b Antibiotics Research and Re-evaluation Key Laboratory of Sichuan Province, Sichuan Industrial Institute of Antibiotics, Chengdu University, Chengdu 610052

Received:2016-04-29 Revised:2016-05-26 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).

1. Synthesis of Antihistamine Drug Hydroxyzine with New N-Alkylation Method.PDF(1692KB)

Abstract

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

Cite this article

Dong Hongbo, Zheng Dengyu, Luo Hongbing, Du Weihong, Lin Jiafu, Cao Shenghua. Synthesis of Antihistamine Drug Hydroxyzine with New N-Alkylation Method[J]. Chin. J. Org. Chem., 2016, 36(11): 2709-2714.

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利用新型氮烷基化方法合成抗组胺药物羟嗪

Synthesis of Antihistamine Drug Hydroxyzine with New N-Alkylation Method

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