Palladium-catalyzed aerobic (1+2) annulation of Csp3–H bonds with olefin for the synthesis of 3-azabicyclo[3.1.0]hex-2-ene

A novel palladium-catalyzed aerobic (1+2) annulation was developed for the synthesis of 3-azabicyclo[3.1.0]hex-2-ene. The palladation of Csp3–H bonds took place twice at the same position in the whole reaction process. Preliminary mechanistic studies by in situ IR revealed that the second C–H palladation and reductive elimination might be slow steps.