This submission belongs to the session b. Combinatorial Synthesis, Parallel Synthesis and Automation of the event The 3rd International Electronic Conference on Synthetic Organic Chemistry
Published date
01 Nov, 1999
Citation
C. Oliver Kappe, Rajender S. Varma, A Novel High-Speed Method for the Generation of 4-Aryldihydropyrimidine Compound Libraries Using a Microwave-Assisted Biginelli Condensation Protocol., in Proceedings of The 3rd International Electronic Conference on Synthetic Organic Chemistry, 1 November–30 November 1999, MDPI: Basel, Switzerland, 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 2
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
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.
Keywords
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