Sequential Synthesis, Olfactory Properties, and Biological Activity of Quinoxaline Derivatives

A simple, practical, and rapid access to quinoxalin-2-ones 1, 1,2,3,4-tetrahydroquinoxalines 2, quinoxalines 3, and quinoxalin-2(1H)-ones 4 has been achieved, based on the copper-catalyzed quinoxalinone formation of 2haloanilines and amino acids followed by their reduction and oxidation. The olfactory properties and lipid accumulation inhibitory activity in cultured hepatocytes of the quinoxaline derivatives were also evaluated.