不对称催化氧化制备(S)-泮托拉唑

Preparation of( S)-pantoprazole by Catalytic Asymmetric Oxidation Reaction

以(2S,3S)-N,N'-二苄基-酒石酸二酰胺和Ti(O-Pri)4形成的手性络合物为催化剂,枯烯过氧化氢为氧化剂,不对称催化氧化制备了(S)-泮托拉唑,转化率87%,纯化后的化学纯度>99.5%,光学纯度99.5%,硫醚含量<0.1%,砜含量<0.1%,其结构经1H NMR确证。

（S）-pantoprazole was prepared by catalytic asymmetric oxidation reaction using chiral titanium complex,formed from （2S,3S）-N,N＇-dibenzyl-tartramide and Ti（O-Pri）4,as the catalyst and cumene hydroperoxide as the oxidant.The conversion was greater than 87％.After purification,the quality of （S）-pantoprazol could be comparable to that of the standard of FDA,with high optical and chemical purity（both ＞99.5％） and low content of thioether and sulphone（both ＜0.1％）.The structure was confirmed by 1 H NMR.