Jun-Ming Li, J. Weng, G. Lu
May 11, 2016
Citations
0
Influential Citations
43
Citations
Journal
Tetrahedron Letters
Abstract
Copper-catalyzed CH sulfonylation of 8-aminoquinoline scaffolds in the unusual C5 position was developed. The protocol using inexpensive CuI as the catalyst and commercially available aryl sulfonyl chlorides as the sulfonylation reagents, shows broad substrate scope, producing moderate to good yield of sulfone. The developed method was conveniently applied to synthesize a potential fluorinated PET radioligand of 5-HT6 serotoninergic receptor. Moreover, mechanistic studies revealed that the reactions underwent a radical process.