Process R&D of Eravacycline: The First Fully Synthetic Fluorocycline in Clinical Development

被引：41

作者：

Ronn, Magnus ^{[1
]}

Zhu, Zhijian ^{[1
]}

Hogan, Philip C. ^{[1
]}

Zhang, Wu-Yan ^{[1
]}

Niu, John ^{[1
]}

Katz, Christopher E. ^{[1
]}

Dunwoody, Nicholas ^{[1
]}

Gilicky, Olga ^{[1
]}

Deng, Yonghong ^{[1
]}

Hunt, Diana K. ^{[1
]}

He, Minsheng ^{[1
]}

Chen, Chi-Li ^{[1
]}

Sun, Cuixiang ^{[1
]}

Clark, Roger B. ^{[1
]}

Xiao, Xiao-Yi ^{[1
]}

机构：

[1] Tetraphase Pharmaceut Inc, Watertown, MA 02472 USA

来源：

ORGANIC PROCESS RESEARCH & DEVELOPMENT | 2013年 / 17卷 / 05期

关键词：

TETRACYCLINE ANTIBIOTICS; ANTIBACTERIAL ACTIVITY; ROUTE;

D O I：

10.1021/op4000219

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

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-Dieckmann 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.

引用

页码：838 / 845

页数：8

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