| 摘要 |
<p>Penzodiazepinones of formula (I):- (where R1, R2, R4 and R5 = H, hal. CF3, (1-7C) o alkyl (1-7C) alkyl or (1-7C) s alkyl, R3 = H, (1-7C) alkyl, lower alkenyl, lower alkynyl, -alkyl (NH(1-7C) alkyl, or alkyl N(alkyl)2, and R6 = H or an N-protecting gp. e.g. PhCH2, aryl SO2 lower alkanoyl, or lower aroyl) are prepd. from isoquinolones of formula IV via the Schmidt or Beckmann reaction to give the caronium ion III, followed by spontaneous addn of H2O giving II and (opt.) substn. of the N atom to give R3 = H. If R6 is protected, the protecting gp. can subsequently be removed. I are of use as muscle relaxants, anti-convulsants and sedatives.</p> |
