手性胺类医药中间体的绿色合成研究进展

Research progress on green synthesis of chiral amine pharmaceutical intermediates

医药生产中普遍存在高污染、高能耗、低效率等问题,急需开发经济、清洁、绿色、低碳的技术。对手性医药中间体进行分类并介绍了含手性胺结构的医药分子,综述了不对称还原胺化法、生物催化法等绿色合成方法应用于手性胺类医药中间体的研究进展,重点阐述了以铵盐、伯胺为氮源的不对称还原胺化法以及利用转氨酶、亚胺还原酶、胺脱氢酶、多酶级联和光-酶级联的生物催化法,并对手性胺类医药中间体领域所面临挑战及发展方向进行了展望。

High pollution,high energy consumption,and low efficiency are common challenges in pharmaceutical production,making the development of economical,clean,green,and low-carbon technologies imperative.Chiral pharmaceutical intermediates were classified,and pharmaceutical molecules containing chiral amine structures were introduced.The research progress on green synthesis methods was reviewed,such as asymmetric reductive amination and biocatalysis,as applied to chiral amine pharmaceutical intermediates.Additionally,the asymmetric reductive amination method with ammonium salt and primary amine as nitrogen sources,as well as the biocatalysis method employing transaminase,imine reductase,amine dehydrogenase,multi-enzyme cascade,and photo-enzyme cascade were explained in detail.Finally,the challenges and development directions in the field of chiral amine pharmaceutical intermediates were discussed.