Synthesis And Analysis Of Organic Compounds With Biological Activities

Nine N' -(4,6-disubstituted pyrimidin-2-yl) -N-cinnamoyl thioureas (III) and seven N' -(4,6-disubstituted pyrimidin-2-yl) -N- dichlorochrysanthemoyl ureas (I) were synthesized from corresponding cinnamic acid and dichlorochrysanthemic acid using PEG-400 as phase transfer catalyst or ultrasonic irradiation, through three steps and four steps respectively. Two 5,7-disubstituted-2-dichlorochrysanthemoylimino-2H-1,2,4-thiadiazolo[2,3-a]pyrimidines (IIa,IIb) were prepared by oxidizing cyclization of N' -(4,6-disubstituted pyrimidin-2-yl) -N- dichlorochrysanthemoyl thiourea. All of these target compounds are new compounds and their structures were confirmed by IR, ~1H NMR and elemental analysis. Their physical properties, spectrum properties, reaction conditions and synthesized methods were discussed as well.The compound N' -(4,6-dimethoxy pyrimidin-2-yl)-N-β -pyridinecarbonyl thiourea (G5q, IV) revealing high lawn-herbicidal activity was analyzed by HPLC, the analytical method in this paper was believable by its good precision and accuracy.The preliminary biological activities test of compounds (I, II) were finished in Shanghai Branch of National Pesticide R&D South Central. The results indicated that some of the target compounds had certain insecticidal activity or fungicidal activity, but not so remarkable was the herbicidal activity. The proliferation effects of compounds (I, III) on K562 cells were finished in Animal Cell & Molecule Biological Lab of Shanghai Normal University. The results displayed that some of the target compounds possessed potential anti-tumor activity by significantly inhibiting proliferation of K562 cells.The structural formulas of the title compounds are as follows respectively:...