盐酸依匹斯汀的合成工艺研究

目的 研究盐酸依匹斯汀的合成工艺.方法以6-氰基-6,11-1H-二苯并[b,e]氮杂(革)为起始原料,经硼氢化钠还原,富马酸盐精制,溴化氰环合得依匹斯汀溴酸盐,用氢氧化钠将其游离,再在乙醇中用盐酸成盐,用乙醇和水重结晶得盐酸依匹斯汀.结果所得的盐酸依匹斯汀的结构经1H-NMR、MS、IR等确证,总收率为55％,HP...

Synthesis technology of epinastine hydrochloride

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.