| 摘要 |
<p>The present invention relates to an improved process for the preparation of Clomipramine salts, particularly Clomipramine hydrochloride of Formula I and Clomipramine sulfate of Formula II. The process for the preparation of Clomipramine hydrochloride of Formula I comprises of reacting 3-chloroiminodibenzyl with N,N-dimethylaminopropyl chloride in an aromatic hydrocarbon in presence of an alkali metal hydroxide; filtering the reaction mixture, cooling, diluting with water and adding aqueous sulfuric acid to obtain crude Clomipramine sulfate; recrystallizing the crude Clomipramine sulfate using acetone-water mixture to obtain Clomipramine sulfate of Formula II having HPLC purity of more than 99.5%; suspending Clomipramine sulfate of Formula II in water, adding an aqueous alkali metal hydroxide solution and an aliphatic hydrocarbon, stirring and separating an aqueous layer and an organic layer; charcoalizing the organic layer, cooling and adjusting pH by addition of alcoholic hydrochloride to yield Clomipramine hydrochloride of Formula I having HPLC purity of more than 99.7%.</p> |
