Green high-yielding one-pot approach to Biginelli reaction under catalyst-free and solvent-free ball milling conditions

Abstract

A simple, green, and efficient approach was used to synthesize 3,4-dihydropyrimidines derivatives. We showed that the application of the planetary ball milling method with a ball-to-reagent weight ratio of 8 for the Biginelli reaction provides 3,4-dihydropyrimidines derivatives with excellent yields (> 98%) in a short reaction time from the one-pot, three-component condensation of aldehydes, ethyl acetoacetate, and urea (or thiourea).