AN OPTIMIZED SYNTHETIC PROTOCOL FOR BIOLOGICALLY RELEVANT, HIGHLY FUNCTIONALIZED BENZOFURANSAbstract
We report here the optimization of an oxidative Michael addition protocol for the synthesis of highly functionalized, biologically relevant benzofurans on gram scale. Rigorous screening of reaction conditions including solvent, atmosphere, base and incubation time, and development of a straight forward precipitation step afforded benzofurans in greater than 95% purity for direct use in biological assays.
Preetpal Singh Sidhu
Department of Medicinal Chemistry and Institute for Structural Biology and Drug Discovery, Virginia Commonwealth University, Richmond, VA 23219, United States of America
12 August, 2013
15 October, 2013
26 December, 2013
01 January, 2014