Concise Synthesis and Antimicrobial Activities of New Substituted 5??Isoxazolpenicillins

XZ Wang, J Jia, Y Zhang, WR Xu, W Liu…

Index: Wang, Xi-Zhao; Jia, Jiong; Zhang, Yan; Xu, Wei-Ren; Liu, Wei; Shi, Fang-Niu; Wang, Jian-Wu Journal of the Chinese Chemical Society, 2007 , vol. 54, # 3 p. 643 - 652

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Citation Number: 7

Abstract

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.