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目的:对R-和S-兰索拉唑的不对称氧化合成反应进行研究。方法:以2-氯甲基-3-甲基-4-(2,2,2-三氟乙氧基)吡啶盐酸盐和2-巯基苯并咪唑为原料,经亲核取代和碱化得中间体2-[[[3-甲基-4-(2,2,2-三氟乙氧基)-2-吡啶基]甲基]硫基]-1H-苯并咪唑,后者经氢过氧化异丙基苯不对称氧化,生成R-和S-兰索拉唑。结果:所制R-和S-兰索拉唑获得结构确证,其总收率均达到65.5%。结论:该法原料利用率高,工艺简单,适用于工业化生产。
Objective: To study the asymmetric oxidation reaction of R- and S-lansoprazole. Methods: 2-Chloromethyl-3-methyl-4- (2,2,2-trifluoroethoxy) pyridine hydrochloride and 2-mercaptobenzimidazole as starting materials, nucleophilic substitution and alkalization The intermediate 2 - [[[3-methyl-4- (2,2,2-trifluoroethoxy) -2-pyridinyl] methyl] thio] -1H-benzimidazole, Asymmetric oxidation of cumene hydroperoxide produces R- and S-lansoprazole. Results: The structures of the obtained R- and S-lansoprazole were confirmed. The total yield reached 65.5%. Conclusion: The method of high utilization rate of raw materials, process is simple, suitable for industrial production.