Process Development of a Novel Azetidinyl Ketolide Antibiotic

…, X Cao, M Coutant, H Dou, K Granskog…

文献索引：Li, Bryan; Magee, Thomas V.; Buzon, Richard A.; Widlicka, Daniel W.; Bill, Dave R.; Brandt, Thomas; Cao, Xiaoping; Coutant, Michael; Dou, Haijian; Granskog, Karl; Flanagan, Mark E.; Hayward, Cheryl M.; Li, Bin; Liu, Fengwei; Liu, Wei; Nguyen, Thuy-Trinh; Raggon, Jeffrey W.; Rose, Peter; Rainville, Joseph; Reilly, Usa Datta; Shen, Yue; Sun, Jianmin; Wilcox, Glenn E. Organic Process Research and Development, 2012 , vol. 16, # 5 p. 788 - 797

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被引用次数: 3

摘要

Process development and the multikilogram synthesis of a novel azetidinyl ketolide antibiotic is described. Starting with clarithromycin, the eight-step synthesis features several telescoped operations and direct isolations, which results in a significant improvement in throughput and a major reduction in solvent usage and waste stream volume over the first scale-up campaign. Particular highlights of this effort include the development of an ...