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

Direct β‑C(sp³)–H Functionalization of Aliphatic Amines to α,β-Unsaturated Imines, Aldehydes, and Chromenes

A metal-free method for direct β-C­(sp³)–H functionalization of aliphatic amine was developed. The method is based on a reaction that yields enamine directly from the corresponding aliphatic amine, which otherwise requires the aid of metallic reagent and/or external oxidant. The reaction is operationally simple, general, and highly efficient in functionalizing both cyclic and acyclic amines. Structurally diverse unsaturated imines were obtained from <i>N</i>-heterocycles, while acyclic amines provided 2-alkyl cinnamaldehyde and benzopyran derivatives with excellent <i>E</i>/<i>Z</i>-selectivity

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

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

Direct β‑C(sp³)–H Functionalization of Aliphatic Amines to α,β-Unsaturated Imines, Aldehydes, and Chromenes

A metal-free method for direct β-C­(sp³)–H functionalization of aliphatic amine was developed. The method is based on a reaction that yields enamine directly from the corresponding aliphatic amine, which otherwise requires the aid of metallic reagent and/or external oxidant. The reaction is operationally simple, general, and highly efficient in functionalizing both cyclic and acyclic amines. Structurally diverse unsaturated imines were obtained from <i>N</i>-heterocycles, while acyclic amines provided 2-alkyl cinnamaldehyde and benzopyran derivatives with excellent <i>E</i>/<i>Z</i>-selectivity

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