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 broug...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.展开更多
基金supported by Program for Innovative Research Team of the Ministry of Education and Program for Liaoning Innovative Research Team in UniversityShenyang Shuangding Pharmaceutical Co.,LTD.,Shenyang,China
文摘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.
