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

Derivatives of N-methylxanthine. II. 8-(p-Carboxyphenyl)theophylline and 8-(p-carboxybenzyl)theophylline

I. Kompiš, J. Mokrý, and J. Tamchyna

Slovak Academy of Sciences, Bratislava

Abstract: cf. C.A. 50, 13947a. The H₂O-insoly. of a great majority of known derivs. of theophylline, substituted at C-8 position, causes difficulty for pharmacol. evaluation. Fusion of 1,3-dimethyl-4,5-diaminouracil with p-MeO₂CC₆H₄CO₂H or p-MeO₂CC₆H₄CH₂CO₂H and cyclization of the acyl deriv. in warm alk. medium gave 8-(p-carboxyphenyl)theophylline (I), unmelted at 360°, and 8-(p-carboxybenzyl)theophylline (II), unmelted at 300°. The alk. salts of I and II are very sol. in H₂O. The properties and synthesis of p-HO₂CC₆H₄CH₂CO₂H, m. 209-11°, from p-MeO₂CC₆H₄CO₂H are described.

Full paper in Portable Document Format: 129a519.pdf (in Slovak)

Chemical Papers 12 (9) 519–524 (1958)