An Improvement for the Synthesis of Clarithromycin

Chin. J. Org. Chem. ›› 2005, Vol. 25 ›› Issue (04): 438-441. Previous Articles Next Articles

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克拉霉素的合成新方法

梁建华，姚国伟*

(北京理工大学生命科学与技术学院北京 100081)

收稿日期:2004-07-15 修回日期:2004-09-12 发布日期:2005-03-30
通讯作者: 姚国伟

An Improvement for the Synthesis of Clarithromycin

LIANG Jian-Hua,YAO Guo-Wei*

(School of Life Science and Technology, Beijing Institute of Technology, Beijing 100081)

Received:2004-07-15 Revised:2004-09-12 Published:2005-03-30
Contact: YAO Guo-Wei

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-hexamethyldisilazane 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 methylation and one-pot deprotection with overall yield 49.5%.

Key words: clarithromycin, silylation, regioselectivity, etherification

Cite this article

LIANG Jian-Hua,YAO Guo-Wei*. An Improvement for the Synthesis of Clarithromycin[J]. Chin. J. Org. Chem., 2005, 25(04): 438-441.

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克拉霉素的合成新方法

An Improvement for the Synthesis of Clarithromycin

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