他汀类药物中间体的生物催化合成研究进展

Advance in biocatalytic synthesis of statin intermediates

他汀类药物是一类重要的降血脂药物,(3R,5S)-二羟基酯是他汀类药物发挥作用的关键结构,也是合成该类药物过程中的重要中间体,因其结构中具有两个手性碳原子,故含有(3R,5S)-二羟基酯结构中间体的制备在某种程度上已成为他汀类药物制备的限速步骤。该文对他汀类药物的类型、作用机制、化学结构和合成路线进行概述。着重对近几年采用生物催化方式制备具有(3R,5S)-二羟基酯结构中间体的方法进行简述。

Statins are major type of cholesterol-lowing drugs, in which the （3R,5S） -dihydroxy esters are key structure and important intermediates for the function and production of statins. Bearing two chiral carbon atoms, the production of （3R ,5S）-dihydroxy esters may be the rate-limiting steps in the statins manufacture. In this paper, the species, mechanisms, structures and synthetic routes of statins were summarized. Several biocatalystic routes for production of （3R,5S）-dihydroxy esters were also reviewed.