摘要
首次报道了利用Raney-Ni催化的氮烷基化方法合成了抗组胺药物羟嗪(Hydroxyzine,1a),在此基础上优化反应条件,对底物进行拓展,成功合成14个二苯甲基哌嗪类化合物,其中包括抗组胺药物去氯羟嗪(Decloxizine,1j)、美克洛嗪(Meclizine,1l)、布克利嗪(Buclizine,1m)与钙离子通道阻滞剂洛美利嗪(Lomerizine,1n),为此方法在这些药物上的首次应用,提高了其在药物合成方面的应用价值.
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.
出处
《有机化学》
SCIE
CAS
CSCD
北大核心
2016年第11期2709-2714,共6页
Chinese Journal of Organic Chemistry
基金
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~~
