A highly diastereo- and enantioselective organocatalytic Michael addition of α-aryl isocyanoacetates to aurone-derived azadienes under mild conditions has been developed. This efficient methodology enables access to chiral α,α-disubstituted α-amino ester derivatives with two adjacent stereocenters, one of them quaternary, bearing a benzofuran scaffold in their structure in high yields and stereocontrol. Furthermore, the reaction product can be readily converted into an α,α-disubstituted α-amino acid in high yield via hydrolysis of the isocyano group without compromising enantioselectivity

中文翻译：

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α-芳基异氰乙酸酯与 Aurone 衍生的氮杂二烯的有机催化非对映和对映选择性迈克尔加成


开发了一种在温和条件下将 α-芳基异氰乙酸酯与 Aurone 衍生的氮杂二烯进行高度非对映和对映选择性有机催化迈克尔加成的方法。这种有效的方法能够以高产率和立体控制获得具有两个相邻立构中心（其中一个是四元立体中心）的手性 α,α-二取代 α-氨基酯衍生物，其结构中带有苯并呋喃支架。此外，通过异氰基的水解，反应产物可以很容易地以高产率转化为α,α-二取代的α-氨基酸，而不影响对映选择性