| 摘要 |
PURPOSE:To obtain a muscle relaxant containing an aminoketone derivative or a salt thereof as an active ingredient. CONSTITUTION:A muscle relaxant obtaining a compound shown by formula I (R1 is p-trihalogenomethyl) or a salt thereof as an active ingredient. The compound shown by formula I as the active ingredient is obtained by reacting 1 equivalent compound shown by formula II with >=0.5 equivalent, preferably 1-10 equivalents formaldehyde and pyrrolidine. The reaction is carried out in the presence of preferably a catalytic amount of an acid, more preferably hydrochloric acid in the absence of a solvent or preferably in a solvent (e.g. alcohol such as propanol, isopropanol, butanol, etc., ketone such as acetone, etc.) at 0-200 deg.C, preferably 10 deg.C- about boiling point of the solvent for 0.5-4hr, preferably 3-48hr. The relaxant may be orally or parenterally administered. A dose is 0.1-20mg/kg/day. The agent has prolonged effects, relaxing action on rigidity in a decerebrate specimen and further anticonvulsant action. |
