School of Cancer and Pharmaceutical Sciences, King's College London, 150 Stamford Street, SE1 9NH, London, UK.
Department of Applied Sciences, Northumbria University, Ellison Place, NE1 8ST, Newcastle upon Tyne, UK.
Org Biomol Chem. 2019 Oct 28;17(40):8982-8986. doi: 10.1039/c9ob01962f. Epub 2019 Oct 4.
A facile microwave assisted three-component protocol allows the synthesis of chiral aryl-1,2-mercaptoamines in water in a few minutes with high yields, bypassing the use of toxic aziridine intermediates. The chiral 1,2-mercaptoamines were then deracemized through enzymatic resolution of the racemates using monoamine oxidase (MAO-N) biocatalysts.
一种简便的微波辅助三组分方案允许在几分钟内在水中高效合成手性芳基-1,2-硫代胺,避免使用有毒的氮丙啶中间体。然后,通过使用单胺氧化酶(MAO-N)生物催化剂对手性外消旋 1,2-硫代胺进行酶促拆分来实现外消旋体的去消旋化。