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

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

References and Notes

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1

Present address: The Beatson Institute for Cancer Research, Garscube Estate, Switchback Road, Bearsden, Glasgow G61 1BD, UK

2

Present address: Hybrigenics, 3-5 Impasse Reille, 75014 Paris, France