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

Abstract

A simple, practical, and rapid access to quinoxalin-2-ones <b>1</b>, 1,2,3,4-tetrahydroquinoxalines <b>2</b>, quinoxalines <b>3</b>, and quinoxalin-2(1<i>H</i>)-ones <b>4</b> has been achieved, based on the copper-catalyzed quinoxalinone formation of 2-haloanilines 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.