Interfacing Microwave Synthesis with Enabling Technologies in Drug Discovery

Doris Dallinger and C. Oliver Kappe, Karl-Franzens University

Date Posted: Thursday, March 30, 2006

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Modern drug discovery steadily relies on high-speed organic synthesis and combinatorial chemistry techniques for the rapid generation of compound libraries. Microwave-assisted organic synthesis in combination with polymer-assisted solution phase (PASP) methods are powerful techniques that are frequently applied in both academia and industry.

Here we report on the rapid synthesis/decoration of privileged heterocyclic scaffolds, namely the dihydropyrimidine (DHPM) scaffold, by applying microwave heating in conjunction with PASP approaches. The use of resin-bound catalysts, reagents and scavengers as well as fluorous reagents in conjunction with microwave heating will be described for amidations, esterifications via a Mitsunobu protocol and N-acylations.

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