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Synlett 2009(11): 1737-1740  
DOI: 10.1055/s-0029-1217373
LETTER
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of 5-Acyl-3,4-dihydropyrimidine-2-thiones via Solvent-Free, Solution-Phase and Solid-Phase Biginelli Procedures

Horacio Comasa, David-Alexandre Buissona, Romain Najmana, Frank Kozielskib, Bernard Rousseaua, Roman Lopez*a
a CEA, LifeScience Division, iBiTec-S, Service de Chimie Bioorganique et de Marquage, Bat. 547, 91191 Gif sur Yvette, France
b Laboratoire des Moteurs Moleculaires, Institut de Biologie Structurale (CEA-CNRS-UJF), 41 Rue Jules Horowitz, 38027,Grenoble Cedex 01, France
Fax: +33(1)58103848; e-Mail: roman.lopez@ymail.com;
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Publication History

Received 20 January 2009
Publication Date:
12 June 2009 (online)

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Abstract

Compounds belonging to the 5-acyl-3,4-dihydropyrimidine-2-thione family were obtained using a solvent-free Biginelli condensation with or without the use of a catalyst. An unprecedented solid-phase procedure involving a polymer-supported aldehyde allowed the preparation of a series of 5-aroyl derivatives starting with crude diketones obtained from their corresponding aryl esters.

Key words

multicomponent reaction - heterocycles - solid-phase synthesis - β-diketones - monastrol