Studies On Palladium Catalyzed Highly Arylation At4-position Of3,4-dihydropyrimidin-2(1H)-ones (DHPMs) Via Ortho C-H Functionalization

In this thesis, a new efficient and simple protocol for the functionalization of3,4-dihydropyrimidin-2(1H)-ones (DHPMs) by palladium catalyzed ortho C-H activation was described.The optimized reaction were obtained when the reaction was conducted in DMF at130℃under air by using Pd(OAc)2as the catalyst and AgOAc as additives with5.0equiv CF3COOH. Under the optimal reaction conditions, the desired products were afforded in moderate to high yield (Scheme1). And all the synthesized products were new and characterized by1H NMR,13C NMR, and HRMS. In addition, the predicted reaction mechanism was also proposed. The steric effect on aryl iodines has a significant influence on the reaction yields.R1=H,m-OCH3,p-OCH3, p-NO2R2=H, p-CH3, p-OCH3, p-Br, p-Cl,o-CH3, O-OCH3, o-NO2Scheme1...