Concise synthesis of dopexamine dihydrochloride via benzyl protecting protocol  

作　　者：Yan Guo Hua Zhang Hao Yan Hai-Long Xin Hong-Yan Shen You-Jun Xu 

机构地区：[1]School of Pharmaceutical Engineering,and Key Laboratory of Structure-Based Drug Design & Discovery (Ministry of Education),Shenyang Pharmaceutical University

出　　处：《Chinese Chemical Letters》2015年第3期357-360,共4页中国化学快报（英文版）

基　　金：supported by Program for Innovative Research Team of the Ministry of Education and Program for Liaoning Innovative Research Team in University;Shenyang Shuangding Pharmaceutical Co.,LTD.,Shenyang,China

摘　　要：Benzyl protecting protocol was first employed in two routes for the concise synthesis of dopexamine dihydrochloride.This protecting group could be cleanly removed under mild condition and no unacceptable ion was brought to the final product.The total yield of route I was 43.8% from phenylacetic acid,while it was 54.1% of route II from 2-（3,4-bis（benzyloxy）phenyl）acetic acid.The titration purity of the final product was more than 99.5%,while any single or total impurities met the known standard of the drug by HPLC analysis.The measured residual palladium met an acceptable limit（〈1 ppm） as an API for injection.Benzyl protecting protocol was first employed in two routes for the concise synthesis of dopexamine dihydrochloride.This protecting group could be cleanly removed under mild condition and no unacceptable ion was brought to the final product.The total yield of route I was 43.8% from phenylacetic acid,while it was 54.1% of route II from 2-（3,4-bis（benzyloxy）phenyl）acetic acid.The titration purity of the final product was more than 99.5%,while any single or total impurities met the known standard of the drug by HPLC analysis.The measured residual palladium met an acceptable limit（〈1 ppm） as an API for injection.

关 键 词：removed protecting titration palladium concise benzyl dissolved concentrated acetic brought 

分 类 号：TQ463[化学工程—制药化工]