Citation: 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 shu

Synthesis of Antihistamine Drug Hydroxyzine with New N-Alkylation Method

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

Corresponding author: Dong Hongbo, bloodwhenseeme@163.com
Received Date: 29 April 2016
Revised Date: 26 May 2016

Fund Project: the Open Foundation of Antibioticis Research and Re-evaluation Key Laboratory of Sichuan Province ARRLKF14-09

Figures(4)

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.
- hydroxyzine,
- drug synthesis,
- Raney-Ni,
- N-alkylation
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通讯作者: 陈斌, bchen63@163.com

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沈阳化工大学材料科学与工程学院沈阳 110142