Department of Chemistry, University of Crete , Vasilika Vouton, 71003 Iraklion, Crete, Greece.
Org Lett. 2018 Feb 16;20(4):1146-1149. doi: 10.1021/acs.orglett.8b00076. Epub 2018 Feb 8.
Asymmetric and site-selective formal [3 + 2]-annulations of γ-alkyl-β,γ-unsaturated γ-lactams with α,β-unsaturated aldehydes have been developed. These organocatalysed transformations yield high value enantioenriched bicyclic γ-lactams with up to four new stereocenters (sometimes including a quarternary carbon). The overall transformation starts from simple and readily accessible furans and oversees a rapid, controlled, and dramatic enhancement in 3D complexity.
已开发出γ-烷基-β,γ-不饱和γ-内酰胺与α,β-不饱和醛的不对称和位点选择性的[3 + 2]-环加成反应。这些有机催化转化反应生成具有高达四个新的立体中心（有时包括一个季碳原子）的高附加值手性双环γ-内酰胺。整个转化过程从简单易得的呋喃开始，并经历了快速、可控和显著的 3D 复杂度增强。
