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

Autor:	Wu-Yan Zhang, Zhijian Zhu, Philip C. Hogan, Magnus Ronn, Chi-Li Chen, John Niu, Yonghong Deng, Christopher E. Katz, Roger B. Clark, Xiao-Yi Xiao, Diana K. Hunt, Cuixiang Sun, Minsheng He, Olga Gilicky, Nicholas Dunwoody
Rok vydání:	2013
Předmět:	Active ingredient Stereochemistry Organic Chemistry Eravacycline Combinatorial chemistry Acylation chemistry.chemical_compound chemistry Cyclohexenone Scientific method Yield (chemistry) Aromatic moiety Physical and Theoretical Chemistry Derivative (chemistry)
Zdroj:	Organic Process Research & Development. 17:838-845
ISSN:	1520-586X 1083-6160
DOI:	10.1021/op4000219
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::8adac5b66737a518fc9a0ca8b62dbae8 https://doi.org/10.1021/op4000219 Zobrazit plný text záznamu