A scalable and expedient route to 1-aza[6]helicene derivatives and its subsequent application to a chiral-relay asymmetric strategy.

A rapid route to diversely functionalized 1-aza[6]helicenes has been achieved via the development of a copper-mediated cross-coupling reaction, followed by PtCl4-catalyzed cycloisomerization. Not only does this method allow access to these functionally important molecules on gram scale, but this strategy is also suitable for relaying the axial chirality of a key intermediate to the helicity of the product.