Process R&D of Eravacycline: The First Fully Synthetic Fluorocycline in Clinical Development
ORGANIC PROCESS RESEARCH & DEVELOPMENT(2013)
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.
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关键词
synthetic fluorocycline,eravacycline,clinical
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