Co~? Catalyzed C-H Activation To Synthesis Potential Pharmaceutical Pyrimidinone Compounds

Nitrogen containing heterocyclic are widely existed in nature,they usually exhibit important pharmaceutical activity and have been extensively applied in medicinal and material science.Pyrimidinone scaffolds which are a well-known class of heterocyclic compounds with significant pharmacological and biological efficiency,including,antitumoral,antiviral,antibacterial activities.Thus,developing the efficient synthesis of novel pyrimidinone is highly demanded in organic synthesis and medicinal chemistry.Comparing to the traditional synthesis,C-H activation methods avoid the protection and deprotection steps and make the synthesis more economic and simpler.Recently,the earth-abundant first-row metal catalyst[Cp*Co?]has received considerable attention due to the cheap cost and comparable catalytic activity.Compared to its Rh and Ir counterparts,[Cp*Co?]exhibits a highest catalytic activity among the Group 9[Cp*M?]complexes in C-H amidation reactions with 1,4,2-dioxazol-5-one.In this study,[Cp*Co?]complexes have been employed as highly efficient catalysts for the C-H activation of 2-substituted acrylamides and coupling with dioxazolones.Amidation of acrylamides,dehydration cyclization and further amidation of pyrimidones could be realized under the suitable reaction conditions.The catalytic system can proceed under good functional group tolerance and high efficiency and selectivity.It provides the efficient method to prepare enamides and pyrimidines.There are six quorum sensing inhibitory pyrimidine compounds.