State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, China.
Org Biomol Chem. 2020 Aug 12;18(31):6162-6170. doi: 10.1039/d0ob01019g.
A facile and efficient strategy to synthesize substituted thiazoles via a cascade reaction from chromone derivatives and thioamides in an environmentally benign medium was developed. This cascade reaction involves a Michael addition/intramolecular cyclization process and a broad scope of reversed regioselectivity products was prepared in a short reaction time with excellent yields. The reversed regioselectivity was also explained by DFT calculations.
开发了一种从色酮衍生物和硫代酰胺在环境友好介质中通过级联反应合成取代噻唑的简便高效策略。该级联反应涉及迈克尔加成/分子内环化过程,在短反应时间内以优异的收率制备了广泛的反区域选择性产物。通过 DFT 计算也解释了反区域选择性。