BENZO[F]QUINOLINONE, METHOD OF ITS SYNTHESIS AND PHARMACEUTICAL COMPOSITION BASED ON THEREOF Russian patent published in 2001 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to benzo[f]quinolinone of the formula (I) where R, R¹ both mean hydrogen atom or combined forming a bond; R² is H, C_1-3-alkyl; R³ is methyl or ethyl; R⁴ and -X-R⁵ each holds one of 7-, 8- and 9-position; R⁴ is H, halogen atom, methyl or ethyl; X means alkyl, alkenyl, alkynyl, a bond, -SO-, -SO₂-, -CO-Y-(CH₂)_n-, -Y-CO-(CH₂)_n-, -CO-, -Z-(CH₂)_n-, SO₃; Y is -S_ , -O-, -NH-; Z is -O-, -S-; n = 0-3; R⁵ means phenyl, naphthalinyl, pyridinyl, pyrazinyl, pyridazinyl, pyrimidinyl, anthracenyl, acenaphthalinyl, thiazolyl, benzimidazolyl, indazolyl, thiophenyl, phenanthrenyl, quinolinyl, fluorenyl, isoquinolinyl (other values are given in p. 1 of the invention claim). Invention relates to also its pharmaceutically acceptable salt that inhibits excessive activity of 5-alpha- -reductase. Invention describes method of synthesis of compounds of the formula (I) and intermediate compounds used for their synthesis. EFFECT: improved method of synthesis, valuable biochemical property. 26 cl, 1 tbl, 292 ex