Synthesis of Kroeurohnke pyridines through iron-catalyzed oxidative condensation/double alkynylation/amination cascade strategy

An efficient protocol for the synthesis of symmetrical and unsymmetrical 2,4,6-trisubstituted pyridines via oxidative cascade annulation of arylacetylenes with benzylamines has been developed. The reaction proceeds smoothly utilizing iron(II) triflate as a catalyst and molecular oxygen as an oxidant with broad substrate scope. Mechanistic studies reveal that the reaction may be experiences an oxidative condensation followed by double alkynylation and amination process. (c) 2021 Elsevier Ltd. All rights reserved.

Automated summary

An efficient protocol for the synthesis of symmetrical and unsymmetrical 2,4,6-trisubstituted pyridines has been developed using iron(II) triflate as a catalyst and molecular oxygen as an oxidant. The reaction proceeds smoothly with a broad substrate scope, undergoing oxidative condensation followed by double alkynylation and amination processes.