Synthesis of novel 5-O-(6′-O-modified)-desosamine 14-membered ketolides |
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作者姓名: | Zhehui Zhao Apeng Wang Xiaoxi Zhang Shuang Yang Zhigang Luo Pingsheng Lei |
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作者单位: | State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Beijing Key Laboratory of Active Substances Discovery and Drugability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China |
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基金项目: | This work was supported by the CAMS Innovation Fund for Medical Sciences (Nos. 2017-I2M-3-011 and 2017-I2M-1-012). And we are grateful to the Department of Instrumental Analysis of our institute for performing the NMR and mass spectroscopy measurements. |
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摘 要: | A new and facile procedure was developed to synthesize novel 5-0- (6′-O-modified)-desosamine 14-membered ketolides by adopting different protective strategies and comparing various glycosylation conditions. Two trichloroacetimidate donors, with Lev or Ac substituent groups at the C-6 position, were synthesized to couple with the erythronolide. Several novel 5-0- (6′-O-modified)-desosamine 14-membered ketolides were obtained to verify the utility of the method.
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收稿时间: | 29 January 2018 |
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