Synthetic study demonstrates sequential difunctionalization of unprotected azacycles using organolithium reagents, highlighting a versatile route to complex substituted amines.
A simple one-pot procedure enables the sequential, regioselective, and diastereoselective introduction of the same or two different substituents to the α- and α'-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.
No takes yet. Share an insight, caveat, or question.
Valles et al. (2021) studied this question.
Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context: