One-Pot Multistep Synthesis of 4-Acetoxy-2-amino-3-arylbenzofurans from 1-Aryl-2-nitroethylenes and Cyclohexane-1,3-diones

Abstract

[reaction: see text] A novel method for synthesizing 4-acetoxy-2-amino-3-arylbenzofurans (4) from 1-aryl-2-nitroethylenes (1) and cyclohexane-1,3-diones (2) is described. The method features one-pot operation of a solution of 1 and 2 in THF with catalytic Et3N (rt, 12 h) followed with Ac2O, Et3N, and DMAP (rt, 5 h), although the process consists of 13 elementary reactions.