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Updated: Oct 1, 2025
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Published on: February 6, 2020
Development of a Practical Synthesis of the 8-FDC Fragment of OPC-167832
Vijayagopal Gopalsamuthiram1, Dang Binh Ho1,2, Cheryl L Peck1
1Medicines for All Institute, Virginia Commonwealth University School of Engineering, Chemical Development 737 N 5th Street, Richmond, Virginia 23298-0100, United States.
Abstract:
A concise and practical synthesis has been developed to provide the 8-fluoro-5-hydroxy-3,4-diydrocarbostyril (8-FDC) fragment of OPC-167832 in 41% yield and in >99% purity over four steps from 3-amino-4-fluorophenol. The key feature of this process is the development of a telescoped one-pot synthesis of the quinolone via a chemoselective amidation/acid-induced cyclization that allows for simple product isolation without the need for column chromatography.
