Organocatalytic Enantioselective Direct Vinylogous Michael Addition of α,β-Unsaturated γ‑Butyrolactam to β‑Acyl Acrylates and 1,2-Diacylethylenes

A highly efficient Michael addition of α,β-unsaturated γ-butyrolactam to various β-acyl acrylates and ene-diones to provide synthetically useful compounds was developed. The products were obtained with high diastereo- and enantioselectivities (up to >25:1 dr and 99% ee) containing adjacent tertiary stereocenters.

本研究开发了一种高效的迈克尔（Michael）加成反应，可将α,β-不饱和γ-丁内酰胺与各类β-酰基丙烯酸酯及烯二酮进行反应，得到具有合成应用价值的化合物。所得产物具备优异的非对映选择性与对映选择性（最高可达dr>25:1、ee值99%），且含有相邻的叔碳立体中心。