Abstract The synthesis of a series of new 5-isoxazolpenicillins is described, which were obtained by coupling substituted isoxazoles with 6-APA. Concise large-scale synthesis of 3, 5-disubstituted isoxazoles by 1, 3-dipolar cycloaddition using copper (I) as catalyst was also investigated. Representative compounds were assayed for antimicrobial activities, showing satisfactory antimicrobial activities against Gram-negative bacteria.
![[3-(4-氟苯基)异恶唑-5-基]甲醇结构式](https://image.chemsrc.com/caspic/387/206055-89-2.png)
![[3-(4-甲氧基苯基)-5-异恶唑基]甲醇结构式](https://image.chemsrc.com/caspic/011/206055-86-9.png)
![[3-(4-氯苯基)-5-异恶唑基]甲醇结构式](https://image.chemsrc.com/caspic/032/206055-90-5.png)
