Supported TBD-assisted solution phase diversification of formyl-aza-heterocycles through alkylation-knoevenagel one pot sequences

A El Maatougui, A Crespo, A MS Silva…

Index: Maatougui, Abdelaziz El; Crespo, Abel; Silva, Artur M.S.; Coelho, Alberto Combinatorial Chemistry and High Throughput Screening, 2011 , vol. 14, # 7 p. 570 - 582

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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.

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