双噻二唑基-α-氨基膦酸酯的合成及其生物活性

Synthesis and Activity of Double Thiadiazole-bsed α-Aminophosphonates

以氨基硫脲为前体,经关环后与1,3-二溴丙烷合成了双1,3,4-噻二唑。再与不同的芳香醛及亚膦酸酯合成了一系列双噻二唑基-α-氨基膦酸酯。所得产品均采用IR、1HNMR、UV、31PNMR及元素分析表征;初步生物活性测试表明,该类化合物对黄瓜灰霉病毒、小麦赤霉病菌、苹果轮纹病毒和水稻纹枯病毒都具有明显的杀菌活性。

Double thiadiazole was synthesized from 5-amino-1, 3,4-thiadiazoles which was previously synthesized from thiosemicarbazide and 1,3-dibromopropane. Subsequently a series of double thiadiazole- based α-aminophosphonates were synthesized by the reaction of the previous product with different aldehydes and phosphates. The structures of these compounds were confirmed by UV, IR, 1HNMR, 31PNMR and elemental analysis. Preliminary bioassay show that they all have excellent fungicidal activity against botrytis cinerea, gibberella zeae,physalospora pinicola and rhizoctonia solani.