The Biginelli reaction, which was first reported more than a century ago, involves the synthesis of 3, 4-dihydropyrimidin- 2(1H)-ones of type 4 by a very simple one-pot condensation reaction of ethyl acetoacetate, benzaldehyde and urea in ethanol. In the past decade, dihydropyrimidine derivatives have exhibited important pharmacological properties, e. g. as the integral backbones of several calcium channel blockers, antihypertensive agents, alpha-1a- antagonists, and neuropeptide Y(NPY) antagonists. In this article, we review development in the Biginelli reaction in the areas such as catalytic synthesis, solid-phase synthesis, microwave irradiation, mechanism and natural products synthesis.

Key words: SOLIDPHASE SYNTHESIS, NATURAL PRODUCTS, MICROWAVE RADIATION, CATALYTIC REACTION, PYRIMIDONE P, SYNTHESIS METHODS