α,α'-C-H Bond Difunctionalization of Unprotected Alicyclic Amines

A simple one-pot procedure enables the sequential, regioselective, and diastereoselective introduction of the same or two different substituents to the alpha- and alpha '-positions of unprotected azacycles. Aryl, alkyl, and alkenyl substituents are introduced via their corresponding organolithium compounds. The scope of this transformation includes pyrrolidines, piperidines, azepanes, and piperazines.

Automated summary

This one-pot procedure allows for the sequential, regioselective, and diastereoselective introduction of the same or two different substituents to the alpha- and alpha'-positions of unprotected azacycles using corresponding organolithium compounds. Various azacycles like pyrrolidines, piperidines, azepanes, and piperazines are included in the scope of this transformation.