有生物活性的哒嗪酮-氨基甲酸酯类衍生物的合成

氨基甲酸酯衍生物;有生物活性的哒嗪酮-氨基甲酸酯类衍生物的合成

Synthesis of Bioactive Pyridazinone-Carbamate Derivatives

Pyridazinone-carbamate derivatives 5a～51 were synthesized starting from 2-substituted4,5-dichloro pyridazinones 1 via two routes. One is that 2-substituted-4-chloro-5-hydroxyl pyridazinones 2 reacted with β-bromoethyl carbamates to afford compounds 5a and 5b. The other is that 2-substituted-4-chloro-5-(2-amino ethyloxyl)pyridazinones 3 obtained from the reaction of 1 with amino ethanol, reacted with chloroformate to give 5a～51. Furthermore, the catalytic hydrogenation of 3 gave 2-substituted-5-(2-amino ethyloxyl)pyridazinones 4, which reacted with chloromates to produce compounds 6a～6d at temperatures between -10～-5 C, and to N,N-dicarbamates 7a and 7b at 0～15 C. The reactivity of intermidiates 3 and 4 was also discussed. The preliminary bioassay indicated that almost all of the compounds showed fungicidal activities.