Verfahren zur Herstellung von Tetracyclinderivaten

摘要

Condensation products of a tetracycline with HCHO and an amine of formula RNH.Z.SO2X where R = H, alkyl or hydroxyalkyl (is not >C4); Z = CH2 or CH2CH2; X = OH when Z = CH2 or X = H or SH when Z = CH2CH2. Compounds are of undetermined structure. "NEW" but tetracyclines are specified as cycline and 7-chloro-6-demethyltetracycline. Stable derivs. having high water solubility useful for oral or parenteral admin. The acute and chronic toxicities are lower than those of the parent tetracycline or their known derivs. The compounds do not cause fatty degeneration of the liver to such a great extent as the parent tetracyclines. Amine: HCHO : tetracycline in ratio 1:1:1 to 1:3:2.