Solid-Phase Synthesis of 4,6-Diaryl-3,4-dihydropyrimidine-2(1H)-one-5-carboxylic Acid Amide Derivatives:A Biginelli Three-Component Condensation Protocol Based on Immobilized beta-Ketoamides

摘要

In 1893,Pietro Biginelli discovered a multicomponent reaction which leads to partly reduced pyrimidinone derivatives(4).Since that time,the "Biginelli reaction" has been known as an efficient one-pot reaction protocol to prepare 3,4-dihydropyrimidine-2(1H)-one(DHPM)derivatives(4).DHPM derivatives are known as interesting heterocyclic scaffolds for drug research.The basic form of the Biginelli reaction is illustrated in Scheme 1.In the past decade,DHPM derivatives with different pharmacological properties were found.The DHPM core structure was found to possess Ca-channel modulating,adrenergic agonistic,mitotic kinesin inhibiting,antibacterial,fungicidal,and other pharmacological properties.