研究鹽酸依匹斯汀的合成工藝。方法 以6-氰基-6,11-1H-二苯并[b,e]氮雜 為起始原料，經(jīng)硼氫化鈉還原，富馬酸鹽精制，溴化氰環(huán)合得依匹斯汀溴酸鹽，用氫氧化鈉將其游離，再在乙醇中用鹽酸成鹽，用乙醇和水重結(jié)晶得鹽酸依匹斯汀。結(jié)果 所得的鹽酸依匹斯汀的結(jié)構(gòu)經(jīng)1H-NMR、MS、IR等確證，總收率為55%，HPLC測(cè)定質(zhì)量分?jǐn)?shù)為99.96%。結(jié)論 本合成工藝穩(wěn)定，條件溫和，操作簡(jiǎn)便，適合鹽酸依匹斯汀的工業(yè)化生產(chǎn)。

To study the synthesis technology of epinastine hydrochloride. Methods Using 11H-dibenzo[b,e]azepine-6- carbonitrile as starting material, epinastine hydrochloride bromate was synthesized by reduction with sodium borohydride, refining with fumaric acid, cyclocondensation by cyanogen bromide. NaOH was used to liberate epinastine hydrochloride bromate and salification was done with HCl in ethanol. And then epinastine hydrochloride was obtained through recrystallisation with ethanol and water. Results The structure of epinastine hydrochloride was confirmed by 1H-NMR, MS, IR, etc, and total yield was 55% with HPLC purity of 99.96%. Conclusion The synthesis technology of epinastine hydrochloride is stable, simple, high productive, and can be applied to industry production.