One-Pot Reactions for Modular Synthesis of Polysubstituted and Fused Pyridines

• DOI: 10.1021/acs.orglett.6b02883
• Publication Date: 2016-10-24T11:56:49Z
• Authors: Zhidong Song; Xin Huang; Wenbin Yi; Wei Zhang
• Keywords: 01 natural sciences; 0104 chemical sciences

A 2-fluoro-1,3-dicarbonyl-initiated one-pot Michael addition/[5 + 1] annulation/dehydrofluorinative aromatization reaction sequence is introduced for regioselective synthesis of di-, tri-, tetra-, and pentasubstituted pyridines as well as fused pyridines. This simple and modular synthesis is performed using readily available starting materials and under transition-metal catalyst-free conditions.