Synthesis And Biological Activity Of Multisubstituted 2-amino-Pyrimidine Derivatives And Their Fuseheterocycle Compounds

Seven S-(+)-N-[3-methyl-2-(4-chlorophenyl) butyryl]-N'-(2-pyrimidinyl) ureas and seven homologous racemism compounds (±)-N-[3-methyl-2-(4-chlorophenyl) butyryl]-N'-(2-pyrimidi-yl) ureas (I) were synthesized from corresponding S-(+)-3-methyl-2-(4-chlorophenyl)butyric acid and (±)-3-methyl-2-(4-chlorophenyl) butyric acid in four steps. Nine new 1-(4,6-substituted pyrimidin-2-yl)-2-thioxo-2,3-dihydropyrido[2,3-d]pyrimidin-4(1H)-one derivatives ( II ) were prepared by the reaction of N-oxide-3-pyridincarbonyl isothiocyanate and 4,6-disubstituted-2-ami-ne pyrimidine. All of these target compounds are new compounds and their structures were confirmed by IR, ¹H NMR and elemental analysis. The physical properties and the spectrum properties of the compounds ( I ),(II) were first reported. The reaction conditions and the synthetic methods were discussed as well. The structural formulas of the title compounds (I ),(II )are as follows respectively:X,Y=CH₃,OCH₃,OC₂H₅,OH,Cl; X,Y can be same or different.In order to investigate the relationship between the structure of compounds and its property. Compound (I d) and (II e) were successfully prepared , their crystal structures were determined by single crystal X-Ray diffraction analysis. And we had some discussion on their structures and activities.The preliminary biological activities tests of target compounds (I ),(II) were all finished in Shanghai Branch of National Pesticide R&D South Central. The results indicated that some target compounds of (I) or (II) series have insecticidal activities, and some target compounds have bactericidal activities and so on mulriple efficacies. The effects test of target compounds (II) on the growth of tumor cells in vitro were finished in Animal Cell & Molecular Biology Lab of Shanghai Normal University. The results indicated that some target compounds (II)...