AN IMPROVED PROCESS FOR PREPARATION OF AMISULPRIDE
The present invention is related to a novel process for the preparation of amisulpride (I) which involves : methylation of 4-amino-salicylic-acid (VI) with dimethyl sulphate and base, optionally in presence of TBAB to obtain 4-amino-2-methoxy methyl benzoate (VII) and (ii) oxidation of 4-amino-2-methoxy-5-ethyl thio benzoic acid (IX) or 4-amino-2-methoxy-5- ethyl thio methyl benzoate (X) with oxidizing agent in the presence of sodium tungstate or ammonium molybdate to give 2-methoxy-4-amino-5-ethyl-sulfonyl benzoic acid (IV) or 2- methoxy-4-amino-5-ethyl-sulfonyl methyl benzoate (XI) respectively.
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Page/Page column 12
(2012/01/06)
Compositions of (S) (-)-amisulpride
A composition is provided comprising an antipsychotic effective amount of (S)(-)-amisulpride, (S)-(-)-4-amino-N-[(1-ethylpyrrolidin-2-yl)methyl]-5-ethylsulfonyl)-2-methoxybenzamide. A preferred composition comprises the (D)-tartrate salt of (S)(-)-amisulpride. The (S)(-) enantiomer exhibits antipsychotic properties and administration of the specific enantiomer reduces adverse side effects by reducing toxicity.
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(2008/06/13)
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