Abstract:
BJECTVIE To study the synthetic method of D-(-)tratrate of (S)-(-)-amisulpride. METHODS (S)-(-)-amisulpride(7) was synthesized from 4-amino-2-methoxy-5-mercaptobenzoic acid via alkylation and oxidation to give 4-amino-2-methoxy-5-ethylsulphonyl benzoic acid(4) which was subjected to condensation with S-(-)-1-ethyl-2-aminomethyl- pyrrolidine(6). Compound 6 was separated from 1-ethyl-2-aminomethyl-pyrrolidine by D-(-)-tartaric acid. The object product (1) was prepared from 7 and D-(-)-tartaric acid via salification with an overall yield of 25% based on 4-amino-2-methoxy-5- mercaptobenzoic acid. RESULTS Chemical structure of product was confimed by element analysis, IR, 1H-NMR and MS. CONCLUSION The process has the advantages of raw material obtained easily, mild reaction, quality controlled easily and suitable for industrial production.