Abstract

An efficient solution-phase parallel procedure to perform the structural diversification of some formyl-nitrogen heterocycles (A) using the reusable TBD supported base is described. The library synthesis is based in a consecutive Alkylation-Knoevenagel functionalisation that uses alkyl halides (B), Michael acceptors (C) and activated methylene compounds (D) as diversity elements.

Keywords: Aza-Michael, Knoevenagel, polymer supported superbases, solution phase synthesis, TBD-Assisted, structural diversification, TBD, Alkylation, alkyl halides, methylene compounds, synthetic organic chemistry, high atom economy