Вид документа : Статья из журнала
Шифр издания : 54/S 98
Автор(ы) : Khudina O. G., Burgart Ya. V., Kravchenko M. A., Saloutin V. I.
Заглавие : Synthesis, structure, tuberculostatic activity, and toxicity of fluoroalkyl-containing 3-hydroxyimino-1,5-benzodiazepines [Electronic resource]
Место публикации : Pharmaceutical Chemistry Journal. - 2011. - Vol. 45, № 2. - С. 75-78
Систем. требования: http://www.springerlink.com/content/51748858760qu110/fulltext.pdf
Примечания : Bibliogr. : p. 78 (11 ref.). - 1.11.2011 г.
ББК : 54
Предметные 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
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Khudina, O. G.; Burgart, Ya. V.; Бургарт Янина Валерьевна; Kravchenko, M. A.; Saloutin, V. I.