目的 对右兰索拉唑的合成工艺进行研究。方法 以4-氯-2,3-二甲基吡啶-N-氧化物为起始原料，经酰化、水解、氯代、取代反应得到兰索拉唑硫醚，再进行不对称氧化、取代反应获得右兰索拉唑。结果 合成右兰索拉唑对映体过量值（ee值）为99.5%，总收率为21.6%。结论 改进后的工艺成本低、操作方法简单、后处理容易、收率高、产物纯度高、可用于工业放大生产。

Objective To study the synthetic technology of dexlansoprazole. Methods Using 4-chloro-2,3-dimethy-pyridine- N-oxide as the starting material, dexlansoprazole was obtained after a series of chemical reactions including acylation, hydrolysis, chlorination, and substitution reaction to give dexlansoprazole sulfide, then asymmetric oxidation and substitution were carried out. Results The total yield with 99.5% enantiomeric excess of dexlansoprazole was up to 21.6%. Conclusion The improved procedure has the advantages of low cost, simple operating procedure, easy post-processing and fine yield. The purity of the product is high and can be scaled up to industrial production.

天津市应用基础与前沿技术研究计划资助项目（11JCZDJC24400）