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Combinatorial Chemistry & High Throughput Screening

Editor-in-Chief

ISSN (Print): 1386-2073
ISSN (Online): 1875-5402

Supported TBD-Assisted Solution Phase Diversification of Formyl-Aza-Heterocycles Through Alkylation-Knoevenagel One Pot Sequences

Author(s): Abdelaziz El Maatougui, Abel Crespo, Artur M.S. Silva and Alberto Coelho

Volume 14, Issue 7, 2011

Page: [570 - 582] Pages: 13

DOI: 10.2174/138620711796367229

Price: $65

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


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