ISSN print edition: 0366-6352 ISSN electronic edition: 1336-9075 Registr. No.: MK SR 9/7 Published monthly

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 H₃₇R_v in experiments in vitro.

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

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