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目的对治疗胃溃疡的质子泵抑制剂右兰索拉唑的合成工艺进行研究。方法以2-巯基苯并咪唑和2-氯甲基-3-甲基-4-(2,2,2-三氟乙氧基)吡啶盐酸盐为原料,在碱性条件下发生威廉姆逊缩合得到兰索拉唑硫醚,兰索拉唑硫醚以钛酸异丙酯/L-(+)-酒石酸二乙酯为催化体系,进行不对称氧化制备右兰索拉唑粗品,该粗品经丙酮-水、异丙醇-正己烷重结晶得到右兰索拉唑精品。结果产品纯度为99.9%,对映体过量值为100%,总收率为38.8%。结论该工艺反应条件温和、操作简便,各步原料价格低廉。
Objective To study the synthesis of dexlansoprazole, a proton pump inhibitor, for the treatment of gastric ulcer. Methods Starting from 2-mercaptobenzimidazole and 2-chloromethyl-3-methyl-4- (2,2,2-trifluoroethoxy) pyridine hydrochloride under basic conditions, Lansoprazole thioether and lansoprazole thioether were synthesized by asymmetric oxidation with isopropyl titanate / L - (+) - diethyl tartarate as catalyst system, The crude product is recrystallized from acetone-water and isopropanol-n-hexane to obtain dexlansoprazole product. Results The product was 99.9% pure with an enantiomeric excess of 100% with a total yield of 38.8%. Conclusion The reaction conditions mild, easy to operate, the raw materials at various steps low prices.