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Antituberculostats. VI. Nucleus-halogenated derivatives of nicotinic acid

M. Čeladník, L. Nováček, and K. Palát

Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Komenský University, Bratislava

 

Abstract: 4-Bromoiiicotinic acid was prepared by the treatment of 4-nitronicotinic acid N-oxide with phosphorus oxybromide. Oxidation of 4-bromo-3-picoline afforded 4-hydroxynicotinic acid exclusively. Analogous reaction of 4-nitronicotinic acid N-oxide with phosphorus oxychloride yielded 4-chloronicotinic acid, which by the reaction with hydroiodic acid afforded 4-iodonicotinic acid. 5-Iodonicotinic acid wras synthetised by the oxidation of 5-iodo-3-picoline, the latter having been obtained in a small yield by a direct iodination of picoline. None of the synthetised compounds, administered in the form of their sodium salts has shown any significant activity against Mycobacterium tuberculosis H37Rv in experiments in vitro.

Full paper in Portable Document Format: 211-2a109.pdf (in Slovak)

 

Chemical Papers 21 (1-2) 109–114 (1967)

Thursday, February 09, 2023

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