| 摘要 |
PURPOSE:To obtain a new compound composed of a pyrazole condensed ring derivative having a specific structure, excellent in inhibiting action on manifestation of androgenic action and therapeutic effects on prostatic hypertrophy, prostatic cancer, etc., and having long duration of activity and high oral absorptivity. CONSTITUTION:A benzoic acid derivative expressed by formula I [R<0> and R<3> are H or lower alkyl; R<1> and R<2> are H, lower alkyl, lower alkoxy, halogen, etc.; (m) is 1 or 2; (n) is 1, 2 or 3] is esterified and then reduced. The produced hydroxyl group is further halogenated and the resultant benzyl halide derivative expressed by formula II (X is halogen) reacts with a cyanogen compound and the formed acetonitrile derivative then reacts with a formic acid ester to afford a compound expressed by formula III, which reacts with semicarbazides to provide a compound expressed by formula IV. The prepared compound further reacts with an orthoformic acid ester to afford the new pyrazole condensed ring derivative, expressed by the formula V (A is CH or N) and capable of inhibiting the manifestation of androgenic action. |
