摘要
对溴甲苯经溴代、N-烷基化得到1-(4-溴苄基)-1H-咪唑,然后与丙烯酸甲酯在?-HPCD作用下经Heck偶联反应得到奥扎格雷甲酯,在碱性条件下水解制得抗血栓药奥扎格雷,总收率为58%。
Ozagrel, an antithrombotic drug, was synthesized from 4-bromotoluene by bromination and N-alkylation to give 1-(4-bromobenzyl)-1H-imidazole which was subjected to Heck coupling reaction with methyl acrylate in the presence of α-HPCD and hydrolysis with an overall yield of 58 %.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2015年第7期674-676,共3页
Chinese Journal of Pharmaceuticals