๐”– Bobbio Scriptorium
โœฆ   LIBER   โœฆ

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

โœ Scribed by Ronn, Magnus; Zhu, Zhijian; Hogan, Philip C.; Zhang, Wu-Yan; Niu, John; Katz, Christopher E.; Dunwoody, Nicholas; Gilicky, Olga; Deng, Yonghong; Hunt, Diana K.; He, Minsheng; Chen, Chi-Li; Sun, Cuixiang; Clark, Roger B.; Xiao, Xiao-Yi

Book ID
120228182
Publisher
American Chemical Society
Year
2013
Tongue
English
Weight
531 KB
Volume
17
Category
Article
ISSN
1083-6160

No coin nor oath required. For personal study only.

โœฆ Synopsis

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.

๐Ÿ“œ SIMILAR VOLUMES

Total Synthesis and Antitumor Activity o
Total Synthesis and Antitumor Activity of ZK-EPO: The First Fully Synthetic Epothilone in Clinical Development
โœ Ulrich Klar; Bernd Buchmann; Wolfgang Schwede; Werner Skuballa; Jens Hoffmann; R ๐Ÿ“‚ Article ๐Ÿ“… 2006 ๐Ÿ› John Wiley and Sons ๐ŸŒ English โš– 600 KB

The clinical success of paclitaxel (PT) in the treatment of ovarian and breast cancer strongly contributed to the assessment that tubulin is one of the best clinically validated targets in tumor therapy. However, one disadvantage with PT and other taxane analogues is their recognition by cellular ef

Cover Picture: Total Synthesis and Antit
Cover Picture: Total Synthesis and Antitumor Activity of ZK-EPO: The First Fully Synthetic Epothilone in Clinical Development (Angew. Chem. Int. Ed. 47/2006)
โœ Ulrich Klar; Bernd Buchmann; Wolfgang Schwede; Werner Skuballa; Jens Hoffmann; R ๐Ÿ“‚ Article ๐Ÿ“… 2006 ๐Ÿ› John Wiley and Sons ๐ŸŒ English โš– 161 KB ๐Ÿ‘ 2 views

**__Nature is a brilliant architect__** for the design of compounds with interesting biological functions. Epothilone B (top), a metabolite of myxobacteria (fruiting body in background), served as the lead structure for the development of an anticancer drug candidate. Optimization efforts led to ZKโ€