Abstract: A novel and simple catalytic methodology to highly efficient synthesis of the 6-isopropyl-3,4-dihydropyrimidines via Biginelli condensation using efficient, eco-friendly 4,5-methano-L-prolines as catalyst under solvent-free condition has been developed. A variety of compounds with excellent biological activity was obtained in good to excellent high yields (up to 99 %) under mild conditions.