| 克拉霉素的合成新方法 |
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| 引用本文： | 梁建华,姚国伟.克拉霉素的合成新方法[J].有机化学,2005,25(4):438-441. |
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| 作者姓名： | 梁建华 姚国伟 |
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| 作者单位： | 北京理工大学生命科学与技术学院,北京,100081 |
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| 基金项目： | 国家经贸委技术创新项目 |
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| 摘 要： | 以醚化剂1-乙氧基环己烯和硅烷化试剂1,1,1,3,3,3-六甲基二硅氨烷为保护试剂, 采用醚化-硅烷化保护法制备了克拉霉素. 以红霉素A肟为原料计算, 经肟羟基醚化、2',4"-OH硅烷化、6-OH选择性甲基化、脱保护至克拉霉素, 四步反应总收率为49.5%.
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| 关 键 词： | 克拉霉素 醚化 硅烷化 区域选择性 |
| 收稿时间： | 2004-7-15 |
| 修稿时间： | 2003年7月15日 |
An Improvement for the Synthesis of Clarithromycin |
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| LIANG Jian-Hua,YAO Guo-Wei.An Improvement for the Synthesis of Clarithromycin[J].Chinese Journal of Organic Chemistry,2005,25(4):438-441. |
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| Authors: | LIANG Jian-Hua YAO Guo-Wei |
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| Institution: | (School of Life Science and Technology, Beijing Institute of Technology, Beijing 100081) |
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| Abstract: | 2',4"-O-bis(trimethylsilyl)erythromycin A 9-O-(1-ethoxycyclohexyl)oxime was prepared for the regioselective methylation by using 1-ethoxycyclohexene as etherification agents and 1,1,1,3,3,3-hexame-thyldisilazane as silylation reagents. Four successive reactions from erythromycin A oxime to clarithromycin were operated in the form of one-pot protection (including etherification and silylation), regioselective me-thylation and one-pot deprotection with overall yield 49.5%. |
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| Keywords: | clarithromycin etherification silylation regioselectivity |
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