Concise Synthesis and Antimicrobial Activities of New Substituted 5‐Isoxazolpenicillins |
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| Authors: | Xi‐Zhao Wang Jiong Jia Yan Zhang Wei‐Ren Xu Wei Liu Fang‐Niu Shi Jian‐Wu Wang |
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| Affiliation: | 1. School of Chemistry and Chemical Engineering, Shandong University, Jinan 250100, P. R. China;2. Tianjin Institute of Pharmaceutical Research, Tianjin 300193, P R. China |
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| 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. |
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| Keywords: | Penicillin Isoxazole Synthesis Antimicrobial activity |
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