S 98 Synthesis, structure, tuberculostatic activity, and toxicity of fluoroalkyl-containing 3-hydroxyimino-1,5-benzodiazepines [Electronic resource] / O. G. Khudina, Ya. V. Burgart, M. A. Kravchenko, V. I. Saloutin // Pharmaceutical Chemistry Journal. - 2011. - Vol. 45, № 2. - P75-78. - Bibliogr. : p. 78 (11 ref.) Рубрики: ХИМИЧЕСКИЕ НАУКИ Аннотация: An improved method for the synthesis of fluoroalkyl-containing 3-hydroxyimino-1,5-benzodiazepines is proposed. For this, 3-hydroxyimines were obtained via nitrosation of 1,3-diketones and 3-oxoesters by tert-butylnitrite in diethylether under acid catalysis conditions and were reacted without isolation and further purification with ortho-phenylenediamine. It was found that polyfluoroalkyl-containing 3-hydroxyimino-1,5-benzodiazepin-2-ones and 2-hydroxy-3-hydroxyimino-2-trifluoromethyl-4-phenyl-1H-1,5-benzodiazepine possess high tuberculostatic activity comparable with that of isoniazide. Tests for acute toxicity of the trifluoromethylated heterocycles showed that they are less toxic than isoniazide \\\\Expert2\\nbo\\Pharmaceutical Chemistry Journal\\2011, 45 (2), 75.pdf |