A Novel High-Speed Method for the Generation of 4-Aryldihydropyrimidine Compound Libraries Using a Microwave-Assisted Biginelli Condensation Protocol.

C. Kappe; Rajender Varma

doi:10.3390/ecsoc-3-01759

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A Novel High-Speed Method for the Generation of 4-Aryldihydropyrimidine Compound Libraries Using a Microwave-Assisted Biginelli Condensation Protocol.

C. Oliver Kappe

^{*

1},

Rajender S. Varma

¹ Institute of Organic Chemistry, Karl-Franzens-University Graz, A-8010 Graz, Austria
² U.S. Environmental Protection Agency National Risk Management Research Laboratory 26 West Martin Luther King Drive, MS 443 Cincinnati, Ohio 45268, USA

Published: 01 November 1999 by MDPI in The 3rd International Electronic Conference on Synthetic Organic Chemistry session Combinatorial Synthesis, Parallel Synthesis and Automation

https://doi.org/10.3390/ecsoc-3-01759

Abstract: In this presentation we report the application of microwave assisted chemistry to the parallel synthesis of 4-aryl-3,4-dihydropyrimidin-2(1H)-ones employing a solventless Biginelli multicomponent condensation protocol. The novel method employs neat mixtures of ß-ketoesters, aryl aldehydes, and urea derivatives with polyphosphate ester (PPE) being used as reaction mediator. Irradiation of these mixtures for 90 s in an unmodified household microwave oven provides dihydropyrimidones in 61-95% yield after aqueous work-up. This protcol was extended towards the parallel synthesis of DHPM compound libraries.

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