Fine chemical production by complementary use of microbial catalysts and organic synthesis

在全合成关键步骤生物催化剂的筛选方面，详细阐述了酶催化反应底物的分子设计。还研究了接近关键中间体的实际合成方案。研究结果表明：1）探索水解酶对糖基衍生物中羟基和酰氧基的区域选择性处理; 2）通过底物特异性研究开发环氧化物水解酶的新功能; 3）合成独特的含氟芳香族物质，探测脂肪酶催化位点的远手性识别。在此基础上，建立了唾液酸酶抑制剂和痕量生物分子手性分析试剂的快速合成路线。

On the screening of biocatalysts for the key steps in the total synthetic schemes, molecular design of substrates for enzyme-catalyzed reactions was thoroughly elaborated. Practical synthetic schemes themselves approaching key intermediates were also studied. As the results, three major methods for preparation were achieved : 1) the exploration of hydrolyzing enzymes which regioselectively treat the hydroxy and acyloxy groups in glycal derivatives ; 2) development of new functions of an epoxide hydrolase through the substrate specificity study ; 3) synthesis of the unique fluorine-containing aromatic substances which probe the recognition of remote chirality in the catalytic site of lipases. Based on them, novel and expeditious synthetic routes for sialidase inhibitors and a chiral analyzing agent for trace amount of biomolecules were established.