依折麦布的合成工艺改进

Improvement on Synthetic Process of Ezetimibe

依折麦布是唯一的胆固醇吸收抑制剂。对3条依折麦布合成路线进行比较分析后,选择了一条反应步骤较短、条件较温和且处理较简单的合成路线,通过核磁共振氢谱和碳谱对中间体进行了表征,并对反应中间体的合成工艺进行了优化,不仅降低了成本而且提高了收率。

Ezetimibe is the only cholesterol absorption inhibitor. Consequently, after comparatively analyzing three synthetic routes of ezetimibe , we selected a synthetic route which possesses the advantages of shorter reac-tion steps , milder conditions , and simpler treatment , characterized the structures of intermediates by 1HNMR and13CNMR, and optimized the synthetic process of intermediates. Therefore , the improved synthetic process of ezetimibe not only lowers the cost but also improves the yield.