Synthesis of 3,4-dihydropyrimidin-2(1H)-one viaRetro-Biginellireaction

摘要

Hydrolytic behavior of 5-acetyl-6-methyl-4-phenyl-3,4-dihydropyrimidin-2(1H)-one under alkaline condition has been explored. Mechanistic details are established by LCMS and HPLC. Evidence suggested that the deacetylative benzylidenation proceeds through the retro-Biginelli reaction. The scope of the retro-Biginelli reaction has been explored by the synthesis of substituted DHPs.