科研之友
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摘要
An organocatalytic asymmetric synthesis of directly linked benzothiazole-dihydroimidazoles with two adjacent tertiary-quaternary stereocenters through a Mannich-type reaction of isocyanoacetates with N-(2-benzothiazolyl)imines is disclosed. When employing bifunctional dihydroquinine-derived squaramide as catalyst, moderate to excellent yields (up to 97 % yield), moderate diastereoselectivities and excellent enantioselectivities (up to >99 % ee) were obtained for a variety of substrates. In addition, the transformation of the resulted directly linked benzothiazole-dihydroimidazole into highly functionalized alpha,beta-diamino esters was also demonstrated.
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单位中国科学院; 华东理工大学
