| 摘要 |
PURPOSE: An intermediate for preparing levosulpiride and a preparation method thereof are provided, thereby preparing levosulpiride in higher yield and purity. CONSTITUTION: An intermediate represented by the formula (V) for preparing levosulpiride of the formula (I) is provided, wherein R1 and R2 are independently hydrogen, C1-C4 lower alkyl or phenyl; R3 is phenyl derivative of the formula (VIII) or naphthyl derivative of the formula (IX); and X is hydrogen or halogen, provided that the formula (V) may be racemic body, (S) body and (R) body because it contains chiral carbon(*). A method for preparing an intermediate of the formula (V) for preparing levosulpiride comprises activating a compound of the formula (IV) in the presence of base using acid anhydride method, acid chloride method or azide method, and reacting the activated compound of the formula (IV) with 2-methoxy-5-sulfamoyl benzoic acid, wherein R1 and R2 are independently hydrogen, C1-C4 lower alkyl or phenyl; R3 is phenyl derivative of the formula (VIII) or naphthyl derivative of formula (IX); and X is hydrogen or halogen.
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