Key Laboratory of Chemical Biology of Hebei Province, College of Chemistry and Environmental Science, and ‡Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of the Ministry of Education, Hebei University , Baoding 071002, People's Republic of China.
Org Lett. 2017 Jul 21;19(14):3943-3946. doi: 10.1021/acs.orglett.7b01860. Epub 2017 Jul 13.
A novel and convenient strategy for the enantioselective synthesis of γ-lactam derivatives via N-heterocyclic carbene catalyzed formal [3 + 2] annulation of enals with 2-aminoacrylates is disclosed. This activation mode provides a complementary approach to the synthesis of various γ-lactam derivatives in good yields with excellent diastereo- and enantioselectivities. In this process, two consecutive stereocenters are constructed, and a quaternary carbon center is also established.
本文报道了一种通过 N-杂环卡宾催化烯醛与 2-氨基丙烯酸酯的形式[3+2]环加成反应，实现γ-内酰胺衍生物对映选择性合成的新颖而简便的策略。这种活化模式为合成各种γ-内酰胺衍生物提供了一种互补的方法，产率高，非对映选择性和对映选择性好。在此过程中，构建了两个连续的立体中心，同时也建立了一个季碳原子中心。
