Synthesis of 5-Aroyldihydropyrimidinones via Liebeskind-Srogl Thiol Ester-Boronic Acid Cross-Couplings

Hana Prokopcová; Leonardo Pisani; C. Oliver Kappe

doi:10.1055/s-2006-958443

LETTER

Synthesis of 5-Aroyldihydropyrimidinones via Liebeskind-Srogl Thiol Ester-Boronic Acid Cross-Couplings

Hana Prokopcová, Leonardo Pisani, C. Oliver Kappe*
Christian Doppler Laboratory for Microwave Chemistry and Institute of Chemistry, Karl-Franzens-University Graz, Heinrichstraße 28, 8010 Graz, Austria
Fax: +43(316)3809840; e-Mail: oliver.kappe@uni-graz.at;

Abstract

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Abstract

A novel and efficient two-step synthesis of 5-aroyl-3,4-dihydropyrimidin-2-ones is reported. These privileged ketone structures are readily generated by microwave-assisted Liebeskind-Srogl-type coupling of boronic acids with the corresponding pyrimidone thiol esters. The thiol esters themselves are easily prepared using Biginelli multicomponent chemistry.

Key words

transition metals - cross-coupling - catalysis - ketones - heterocycles

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References

References and Notes

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