Enantioselective Alkylation of Fused Bicyclic Pyridines Enabled by Chiral Lithium Amides as Traceless Auxiliaries

Pyridines and nitrogen containing heterocycles comprise a large portion of pharmaceutical compounds and have many practical applications. Herein, we describe a straightforward, enantioselective method for direct alkylation of fused bicyclic pyridines, using chiral lithium amides as traceless auxiliaries. This method is tolerant of a variety of activated electrophiles which can allow for further functionalization.