Microwave‐Assisted Tandem Kornblum Oxidation and Biginelli Reaction for the Synthesis of Dihydropyrimidones
Asif A. Malik, Nisar A. Dangroo, Tabassum Ara
Abstract
Abstract A simple and straightforward approach for the synthesis of dihydropyrimidones via sequential Kornblum oxidation/Biginelli reaction has been developed. The protocol involves an in situ oxidation of benzyl halides which serve as a carbonyl equivalents followed by cyclocondensation with (thio) urea and ethylacetoacetate to furnish dihydropyrimidones under catalyst and base free conditions in a one‐pot tandem manner under microwave irradiation. Further, the product purification using aqueous recrystallization avoids large quantities of volatile and a toxic organic solvent usually required for work‐up and very less time required for this process makes the method environmental‐ and nature‐friendly.