2-〔4(s)-4-酚胺基-3-氧代-2-异噁唑烷基〕-5-氧代-2-四氢呋喃甲酸钠类化合物的合成

SYNTHESIS OF SODIUM 2-[4(S)-4-AMIDO-3-OXO-2-ISOXAZOLIDINYL]-5-OXO-2-TETRAHYDROFURANCA-RBOXYLATE

以L-丝氨酸和α-酮戊二酸为原料,采用三条合成路线,经6～8步反应,合成8个目标化合物。其部份中间体的结构经IR,PMR,MS及元素分析证实。产物的结构也经IR及PMR证实。体外抑菌试验表明,TM7和TM8显示较强的广谱抑菌活性,TM6则具有中等强度。TM2和TM3对金葡菌也有一定活性。

Eight target compounds of sodium 2-[4 (s)-4-amido-3-oxo-2-isoxazolidiny] -5-oxo-2-tetrahydrofurancarboxylate have been suc-essfully synthesized with 3 routes in 6~8 steps from L-serine and alpha-keto-glutaric acid. Their chemical structures have been identified with IR, PMR, MS and elementary analysis.Antibacterial activities of the target compounds have been tested in vitro. TM7 and TM8 have highly activities against Gram-negative and Gram-positive bacteria. TM6 has moderate strength. TM2 and TM3 have also define strength against S. aures.