Synthesis of several novel 14-membered ketolides bearing modified 5-O-4′-[1,2,3] triazol desosamine side chain |
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| Authors: | Xiaozhuo Chen Yanpeng Xu Zhehui Zhao Pingsheng Lei |
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| Institution: | State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Chinese Academy of Medical Sciences, Beijing 100050, PR China; Beijing Key Laboratory of Active Substances Discovery and Drug Ability Evaluation, Chinese Academy of Medical Sciences, Beijing 100050, PR China; Department of Medicinal Chemistry, Institute of Materia Medica, Peking Union Medical College, Chinese Academy of Medical Sciences, Beijing 100050, PR China |
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| Abstract: | 4-Azido modified desosamine 4a was synthesized and coupled to erythronolide 9. Using trichloroacetimidate donor in the presence of TMSOTf was considered as the most efficient condition for the glycosylation reaction. Five novel 14-membered ketolides 12a–e bearing modified 5-O-4′-1,2,3] triazol desosamine side chain were synthesized by the azide/alkyne click chemistry method. |
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| Keywords: | Desosamine Ketolide Glycosylation Click chemistry Antibiotics |
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