An Efficient and Scalable Synthesis of Quinolone 006

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  • Huang Xiao-guang
    Department of API Research and Development, Guangzhou Baiyunshan Tianxin Pharmaceutical Co., Ltd.
  • Chen Kun-nan
    Department of API Research and Development, Guangzhou Baiyunshan Tianxin Pharmaceutical Co., Ltd.

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Abstract

<p>Quinolone 006 is under development as an anti-methicillin-resistant Staphylococcus aureus quinolone antibiotic. A linear synthetic route was utilized to prepare the compound on a multi-kilogram scale with an overall yield of 71%. The process was optimized by controlling the temperature and the vacuum pressure. Examples of parameters examined in an effort to control the polymorphism of the 006 active pharmaceutical ingredient are described.</p>

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