Microwave-Assisted Scavenging of Electrophiles Utilizing Polymer-Supported Sequestration Reagents
Poster Jun 22, 2006
Doris Dallinger and C. Oliver Kappe
In recent work we have reported the automated generation of a diverse library of multifunctional dihydropyrimidines (DHPMs) utilizing a microwave-mediated solution phase Biginelli three component condensation.
Since most of the pharmacologically attractive DHPM derivatives are N3-acylated analogs, we became interested in developing a rapid method for accessing libraries containing this structure motif in high-throughput format.
We now present the high-speed scaffold decoration of the library, introducing a new point of diversity at the N3 position. Different scavenging techniques using polymer-supported sequestration agents are described for the purification steps in the synthesis of N3-acylated dihydropyrimidines.
The Pathogen Box: A Catalyst for Neglected Disease Drug DiscoveryPoster
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Selective Debenzylation of N-Benzyloxypyrazinones in FlowPoster
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The Prestwick Chemical Library® (PCL) is Prestwick’s flagship product dedicated to screening. It is a collection of 1280 molecules comprising 100% approved drugs (FDA, EMEA and other agencies) selected for their high chemical and pharmacological diversity. The PCL was designed to reduce the risk of "low quality" hits and therefore the cost of the initial screening, and appears to be an efficient smart library for hit discovery. The PCL comes with an extended fully-annotated database.READ MORE