【摘要】 <正> 许多噻唑类化合物具有生物活性,有些已作为杀菌剂、除草剂在农业上得到应用。近年来还进行了α-氨基酸的类似物α-氨基膦酸的合成及其生物活性的研究。迄今为止,还未见有4-噻唑基膦酸酯类化合物的合成和生物活性方面的文献报道。本文报道一系列2-氨基-5-取代-4-噻唑基膦酸酯(1)和2-氨基-4-取代-5-噻唑基膦酸酯(2)的合成。这类化合物显示了一定的杀菌活性。 1由取代乙酰氯与亚磷酸三酯经Arbuzov反应得到的取代乙酰基膦酸三酯(3)与缩二硫脲的溴氢酸盐(4)、一定量的弱碱(如硫脲、乙酸钾)在乙醇中反应制得。溶剂和碱的强弱更多还原

【Abstract】 A series of dialkyl 2-amino-5-substituted-4-thiazolyl phosphonates（1） have beensynthesized by the reaction of the substituted acetyl phosphonates （3） with formidinedisulfide dihydrobromide （4）. Two derivatives of compound 1 were prepared. However,the reaction between 2-substituted-2-oxo-ethyl phosphonate （5）and compound 4 wascarried out under similar condition, affording the expected product 2-amino-4-substituted-5-thiazolyl phosphonate （2） only with low yield. The effects of thesubstituent in thiazole ring throuth bonding and nobonding interactions are indicatedby studying ¹H and ³¹P NMR of the compound 1 and 2. A series of substituted acetylphosphonates （3） ware prepared as synthetic intermediate. The keto-enol tautomerism ofcompound 3 was studied by ¹H and ³¹P NMR.更多还原