Process R&D of Eravacycline: The First Fully Synthetic Fluorocycline in Clinical Development
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- 作者：Magnus Ronn ; Zhijian Zhu ; Philip C. Hogan ; Wu-Yan Zhang ; John Niu ; Christopher E. Katz ; Nicholas Dunwoody ; Olga Gilicky ; Yonghong Deng ; Diana K. Hunt ; Minsheng He ; Chi-Li Chen ; Cuixiang Sun ; Roger B. Clark ; Xiao-Yi Xiao
- 刊名：Organic Process Research & Development
- 出版年：2013
- 出版时间：May 17, 2013
- 年：2013
- 卷：17
- 期：5
- 页码：838-845
- 全文大小：314K
- 年卷期：v.17,no.5(May 17, 2013)
- ISSN：1520-586X
文摘
Process research and development of the first fully synthetic broad spectrum 7-fluorotetracycline in clinical development is described. The process utilizes two key intermediates in a convergent approach. The key transformation is a Michael鈥揇ieckmann reaction between a suitable substituted aromatic moiety and a key cyclohexenone derivative. Subsequent deprotection and acylation provide the desired active pharmaceutical ingredient in good overall yield.