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Synthesis of novel 5-O-(6′-O-modified)-desosamine 14-membered ketolides
作者姓名:Zhehui Zhao  Apeng Wang  Xiaoxi Zhang  Shuang Yang  Zhigang Luo  Pingsheng Lei
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
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.
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.

收稿时间:29 January 2018
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