3,4-二氢嘧啶-2 -酮衍生物合成研究进展

报道了最近6年来3,4二氢嘧啶酮衍生物合成研究进展,包括催化合成法、绿色合成法以及天然产物合成中的一些研究进展,为该类化合物的合成提供了详尽的文献综述。有望在药物合成、不对称合成和天然产物合成方面提供有意义的指导。

Recent Progresses in the Synthesis of 3, 4-Dihydropyrimidinones

The Biginelli reaction,which was first reported more than a century ago,involves the synthesis of 3,4-dihydropyrimidin2-(1-H)-ones of type 4 by a very simple one-pot condensation reaction of ethyl acetoacetate,benzaldehyde and urea in ethanol.In the past six years,dihydropyrimidine derivatives have exhibited important pharmacological properties,e.g.as the integral backbones of several calcium channel blockers,antihypertensive agents,alpha-1-antag-onists,and neuropeptide Y(NPY)antagonists.In this article,we review the development on the Biginelli reaction in the areas such as catalytic synthesis,green synthesis,asymmetric synthesis and natural products synthesis.