Synthesis Of Novel N-alkylated3,4-dihydropyrimidinone-C₆₀

Fullerene has been paid more attention for its special structure and the promisingbiological activities, such as antibacterial, anti-HIV virus, DNA-cleaning, antitumorand inhibition of enzyme activity. It is important in antibacterial that C60has strong π-πinteraction and can be combined with biological target molecules, which exhibitsexcellent biological activities.3,4-dihydropyrimidine-2-(1H)-ones are a kind ofcompounds with heterocyclic structure and pharmacological properties, which not onlyinterfere the synthesis of DNA by blocking the synthesis and exchange of deoxidationof pyrimidine nucleoside, but also has antibacterial, antihypertension activities, and soon. As studies show that N-functional DHPM usually have more excellentpharmacological activities. N-alkyl-DHPM compounds also have an impact onthe synthesis of DNA through alkylation with DNA. With the method of drug design tosuperimposed subunits, we synthesize novel N1-alkylated-DHPM-C60derivatives, andstudy the optical properties and biological activities in order to obtain the compoundswith higher bioavailability, which has important significance for the development ofthe new drug.The main research contents are as follows. Firstly, synthesized a series of DHPMderivatives through Biginelli reaction, and studied the biological activities to get thecompounds with higher antibacterial activity. Secondly, designed and synthesized23kinds of N1-alkyl-DHPM compounds. Thirdly, designed and synthesized25kinds ofintermediate products. Finally, designed and synthesized25kinds of novelN-alkyl-DHPM-C60pyrrolidine compounds, and studied their optical properties andbiological activity in order to obtain novel compounds with higher antibacterialactivity. The target products and intermediate compounds were confirmed by1H NMR,13C NMR, HSQC, HMBC, HR-MS, IR and UV-vis.