Synthesis And Biological Activity Of Multisubstituted 2-amino-Pyrimidine Derivatives And Their Fused Heterocycle Compounds(Ⅵ),(Ⅶ)

Eighteen N'-(substituted pyrimidin-2-yl)-N- P -(or y -)pyridinecarbonyl thioureas( I ), (II ), five (+)-trans-chrysanthemoyl thioureas( V ) and five dichlorochrysanthemoyl thioureas(VI) were synthesized from corresponding P -(or y -)pyridinecarbonic acid, (+)-trans-chrysanthemic acid and dichlorochrysanthemic acid in four steps. Fourteen 2- P -(or Y -)pyridinecarbonylimino-2H-l, 2, 4-thiadiazolo[2, 3-a]pyrimidines(III), (IV) were prepared by oxidizing cyclization of -(or -)pyridinecarbonyl thioureas( I ), (II). All of these target compounds are new compounds and their structures were confirmed by IR, !HNMR and elementary analysis. Their physic-chemical properties, spectrum properties, reaction conditions and synthetic methods were discussed as well. The structural formulas of the title compounds are as follows respectively:The preliminary biological activities test of ( I )^VI six series target compounds were all finished in Shanghai Branch of National Pesticide R&D South Central. The results indicated that some target compounds of ( I )^IV series have excellent herbicidal activities, and a good regulating activity for corn's growth; some target compounds of (V)^VI series have herbicidal activities, insecticidal activities, bactericidal activities and so on mulriple efficacies.