Development of a Practical Synthesis of the 8-FDC Fragment of OPC-167832.

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.

SUBMITTER: Gopalsamuthiram V 

PROVIDER: S-EPMC8892917 | biostudies-literature | 2022 Mar

REPOSITORIES: biostudies-literature