目的 對右蘭索拉唑的合成工藝進行研究。方法 以4-氯-2,3-二甲基吡啶-N-氧化物為起始原料，經(jīng)?；?、水解、氯代、取代反應得到蘭索拉唑硫醚，再進行不對稱氧化、取代反應獲得右蘭索拉唑。結(jié)果 合成右蘭索拉唑?qū)τ丑w過量值（ee值）為99.5%，總收率為21.6%。結(jié)論 改進后的工藝成本低、操作方法簡單、后處理容易、收率高、產(chǎn)物純度高、可用于工業(yè)放大生產(chǎn)。

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.

天津市應用基礎與前沿技術研究計劃資助項目（11JCZDJC24400）