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Microwave-Assisted Scavenging of Electrophiles Utilizing Polymer-Supported Sequestration Reagents

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.