2-芳基-3-N-丙酰基-5-(2-溴-4-氟苯基)-1,3,4-噁二唑啉类衍生物的合成及抗菌活性

Synthesis and Antibacterial Activities of 2-Aryl-3-N-Propanoyl-5-(2-Bromo-4-Fluorophenyl)1,3,4-Oxadiazoline Derivatives

2-溴-4-氟苯甲酰肼(1)与芳香醛缩合得到酰腙(2a^2i),再与丙酸酐环反应合成了9种新型的2-芳基-3-N-丙酰基-5-(2-溴-4-氟苯基)-1,3,4-二唑啉类衍生物(3a^3i),收率79%~84%。化合物的结构经元素分析、IR、1HNMR和MS确证。初步的抗菌试验表明,部分目标化合物表现出较好的抑菌活性。

Condensation of 2-bromo-4-fluorobenzoyl hydrazine （1） with aromatic aldehydes produced corresponding hydrazones（2a-2i）. Cyclization of 2a-2i with propanoic anhydide gave the title compounds 3a- 3i in good yields of 79.3% -85.5 %. Their structures were characterized by means of elemental analysis, IR, 1^H NMR and MS spectra. The preliminary antibacterial tests showed that most of them had good antibacterial activities.