2-氨基取代噻唑基膦酸脂的合成

本文报导一系列2-氨基-5-取代-4-噻唑基膦酸酯和2-氨基-4-取代-5-噻唑基膦酸酯的合成. 这类化合物显示了一定的杀菌活性.

Synthesis of dialkyl-2-amino substituted thiazolyl phosphonates

A series of dialkyl 2-amino-5-substituted-4-thiazolyl phosphonates I (R = CO2Et, cyano, (un)substituted Ph; R1 = Et, Me2CH) have been synthesized by the reaction of the substituted acetyl phosphonates II with formamidine disulfide dihydrobromide (III). However, the reaction between BzCH2P(O)(OEt)2 and III was carried out under similar condition, affording the expected product 2-amino-4-substituted-5-thiazolyl phosphonate IV only with low yield. The effects of the substituent in thiazole ring through bonding and nonbonding interactions are indicated by studying 1H and 31P NMR of the compounds I and IV. A series of substituted acetyl phosphonates II were prepared as synthetic intermediate. The keto-enol tautomerism of compound II was studied by 1H and 31P NMR.