3,4-二氢嘧啶-2-酮衍生物合成研究进展

Recent Advance in the Synthesis of 3,4-Dihydropyrimidinones

综述了近十年来 3,4 二氢嘧啶 2 酮衍生物合成的研究进展 ,包括催化合成、固相合成、微波促进合成及天然产物合成中的一些最新研究进展。

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.