Study On The Synthesis Of Spirooxindole Derivatives And Pyrimidinones Derivatives

Multicomponent reactions (MCRs) have received widespread concern by virtue of their high efficiency, high productivity, simple operation, and high atomic economy etc. It has become a powerful tool for generating libraries of molecules for the discovery and structural optimization of biologically active leads and potential drug candidates. In line with the principle of green and atom economy, we studied the research of the multicompont synthesis of a new structure of spiro [indoline-pyrrolo[1,2-c]imidazole] derivatives in water,while we change the traditional synthetic route, the first time report synthesis of pyrimidinone derivatives catalyzed by CAN (cerium (IV) ammonium nitrate) under solvent-free conditions.Part1:One-pot Synthesis of Spirooxindole Derivatives in WaterThe spirooxindole derivatives widely exist in some natural products. It has been the focus of considerable attention due to their significant biological activities and pharmacological activities. An efficient methodolody for synthesis of new skeleton of spiro[indoline-pyrrolo[1,2-c]imi-dazole] via one pot three-component reactions of isatins, malononitrile, and hydantoin in water is described. The reaction is environmental friendly, excellent yields, and follows a easy work-up procedures.Part2:One-pot Synthesis of Pyrimidinone Derivatives Catalyzed by CANResearch indicated that some of the3,4-dihydropyrimidine-2-one compounds (DHPMs) has significant pharmacological activities. Moreover, srveral DHPMs have functions of antivirus, antiseptic and antiphlogistic. Therefore, the synthesis of pyrimidinone core gained considerable attention. A simple and efficient method has been developed for the synthesis of pyrimidinone derivatives through a Biginelli-type three-component condensation of various aldehydes, cyclopentanone and urea or thiourea in the presence of cerium (IV) ammonium nitrate (CAN). This process offered one way to afford pyrimidinones in good to excellent yields, with a simple procedure and short reacton time.