Asymmetric Reductive and Alkynylative Heck Bicyclization of Enynes to Access Conformationally Restricted Aza[3.1.0]bicycles
Xiaolei Huang, Minh Hieu Nguyen, Maoping Pu, Luoqiang Zhang, Yonggui Robin, Yun‐Dong Wu, Jianrong Steve Zhou
Abstract
Conformationally restricted azabicycles are becoming increasingly important in medicinal research. Asymmetric Heck bicyclization of enynes proceeds to give medicinally useful aza[3.1.0] and aza[4.1.0] bicycles with excellent enantioselectivity. The key organopalladium species after bicyclization can be trapped by silanes and terminal alkynes.
Topics & Concepts
OrganopalladiumHeck reactionSilanesChemistryCombinatorial chemistryAsymmetric hydrogenationStereochemistryEnantioselective synthesisCatalysisPalladiumOrganic chemistrySilaneCatalytic C–H Functionalization MethodsCatalytic Cross-Coupling ReactionsCatalytic Alkyne Reactions