酶法制备手性芳香胺化合物的研究进展

Progress in enzymatic production of chiral arylamines

手性芳香胺是药物合成的重要中间体,同时也可用作手性助剂及手性拆分剂。本文综述了近年来国内外酶法制备手性芳香胺化合物的研究进展,包括脂肪酶催化的选择性酰胺化反应和转氨酶催化的不对称合成、拆分反应。并展望了其今后研究发展的方向:使用脂肪酶催化时可以研究动态动力学拆分来提高产率;使用转氨酶催化时可以尝试研究辅酶再生系统以降低成本,还可以通过反应体系和工艺路线进行改进以提高反应效率。

Optically pure arylamines are important building blocks in drug synthesis and are commonly used as chiral auxiliaries and chiral resolving agents.Recent development in the enzymatic synthesis of enantiopure arylamines was reviewed in this paper,including lipase-based enantioselective acylation,transaminase-based asymmetric synthesis and kinetic resolution.Prospects of biocatalysts application in chiral amine synthesis were also discussed.Dynamic kinetic resolution might be a possible way to improve the yield of lipased-catalysed acylation,while the study of coenzyme regeneration system might reduce the cost in transaminase-catalysed reaction.Improvements in reaction system and process might also greatly enhance the efficiency of transaminase-catalysed reaction.