You are here:
A NOVEL HIGH-SPEED METHOD FOR THE GENERATION OF 4-ARYLDIHYDROPYRIMIDINE COMPOUND LIBRARIES USING A MICROWAVE-ASSISTED BIGINELLI CONDENSATION PROTOCOL -
Citation:
Kappe, C. O. AND R S. Varma*. A NOVEL HIGH-SPEED METHOD FOR THE GENERATION OF 4-ARYLDIHYDROPYRIMIDINE COMPOUND LIBRARIES USING A MICROWAVE-ASSISTED BIGINELLI CONDENSATION PROTOCOL -. Third International Electronic Conference on Synthetic Organic Chemistry, Internet, 9/1-30/1999.
Description:
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 B-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 protocol was extended towards the parellel synthesis of DHPM compound libraries.