General protocols for the N-functionalization of 1,2-azaborines with C(sp3), C(sp2), or C(sp) electrophiles are described. The syntheses of a new parental BN isostere of trans-stilbene and a BN isostere of a lisdexamfetamine derivative were accomplished with the developed methodology.
Keywords: BN heterocycles; N-functionalization; amination; azaborines; cross-coupling.