Parallel Scale-up of the Biginelli Cyclocondensation

The Biginelli dihydropyrimidine synthesis is a simple but powerful one-pot three-component cyclocondensation involving ureas, aldehydes and CH-acidic carbonyl compounds. The synthesis of structures with the dihydropyrimidine (DHPM) scaffold has become of certain interest during the last years as DHPMs show widespread biological and pharmaceutical activities.


An effective and rapid protocol to produce numerous DHPM derivatives has attracted considerable interest. Microwave-mediated parallel synthesis allows generating various DHPMs within only one run in multigram scale.

Herein the parallel synthesis of different bromophenyl-DHPMs suitable for further scaffold decorations to introduce broader diversity into the basic structure is presented.

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