Study On Synthesis And Characterization Of Impurities Of Drotaverin Hydrochloride

Drotaverin hydrochloride is a very efficient antispasmodic and its effect was produced by direct action on smooth muscles.The total export of drotaverin hydrochloride made by Zhejiang Apeloa Pharmaceutical Co.Ltd.reaches almost ten tons per year.But because of REACH, drotaverin hydrochloride of Zhejiang Apeloa is facing the problem of impurities exceeded the limits of REACH.To improve economical benefit,to enlarge export of drotaverin at EU market and to reduce pressure which brought by the cost of detection,we need to know the structures of impurities, provide synthetic methods of relevant substances,to modify the original process of drotaverin and to do research on toxicology when necessarily.This dissertation undertook the work of synthesis and identification of impurities of drotaverin,which occupy more than 0.15%.Finally,we synthesized five target compounds by means of reference paper.Being analyzed by HPLC,we proved that the impurity No.1 is mixtures of 1-(3-ethoxy-4-hydroxybenz yl)-6,7-diethoxy-3,4-dihydroisoquinoline hydrochloride(Qâ… )and 1-(3,4-diethoxybenzyl)-6-ethoxy -7-hydroxy-3,4-dihydroisoquinoline hydrochloride(Qâ…£).The impurity No.2 is 1-(4-ethoxy-3-hydroxybenzyl) -6,7-diethoxy-3,4-dihydroisoquinoline hydrochloride(Qâ…¡)and the impurity No.6 is drotaveraldine(Qâ…¤).