Solvent free one-pot multi-component synthesis of β-azaarene substituted ketones via a Sn-catalyzed C(sp3)–H functionalization of 2-alkylazaarenes

Abstract

A tin-catalyzed solvent free one-pot multi-component cascade reaction strategy for the direct Michael addition/C(sp³)–H functionalization of 2-alkylazaarenes with aldehydes and ketones via an aldol reaction has been developed. This is the first report and provides cost effective new access to potent biologically/medicinally important azaarene derivatives with high atom economy.