Metal Free C-H Functionalization Enabled Diastereoselective Multicomponent Reaction of N-Heterocycles to Fused Heteropolycycles.

A novel C-H functionalization enabled multicomponent reaction involving N-heterocycles, dinucleophile, and dipolarophile has been developed. Direct α- and more challenging β-C(sp3)-H functionalization of aliphatic N-heterocycles was achieved without the use of metallic reagents and oxidants under either conventional or microwave aided heating conditions. In a single operation, up to five carbon-carbon and carbon-heteroatom bonds are formed in a highly diastereoselective manner, providing the expeditious access to the complex heteropolycycles.