Copper mediated C–H amination with oximes: en route to primary anilines

Abstract

Here we report an efficient Cu(I)-mediated C–H amination reaction with oximes as amino donors to introduce NH₂ groups directly. Various strongly coordinating heterocycles including quinoline, pyrimidine, pyrazine, pyrazole and triazole were tolerated well. The potential utility was further demonstrated in a late-stage modification of telmisartan (an antagonist for the angiotensin II receptor).