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METHOD FOR MANUFACTURING 5-(HYDROXY-PROTECTED)-5-(SUBSTITUTED OR UNSUBSTITUTED)2,3-ANHYDRO-2-DEOXYURIDINE COMPOUND
METHOD FOR MANUFACTURING 5-(HYDROXY-PROTECTED)-5-(SUBSTITUTED OR UNSUBSTITUTED)2,3-ANHYDRO-2-DEOXYURIDINE COMPOUND
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机译:制造5-(羟基保护的)-5-(取代或未取代的)2,3-脱水-2-脱氧尿苷化合物的方法
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摘要
PURPOSE: Provided is a method for manufacturing 5-(hydroxy-protected)-5-(substituted or unsubstituted)2,3-anhydro-2-deoxyuridine compound in a high yield which is useful as an intermediate of a compound useful in treating acquired immune deficiency syndrome (AIDS). CONSTITUTION: The method for manufacturing 5-(hydroxy-protected)-5-(substituted or unsubstituted)2,3-anhydro-2-deoxyuridine compound is characterized by the next step of: reacting 5-(hydroxy protected)-5-(substituted or unsubstituted)-2-deoxyuridine of the formula (4) with 1,1-sulfonyldiimidazole of the formula (3) in the presence of base and polar or nonpolar organic solvent at 0-150 deg.C, preferably 25-90 deg.C. Optionally, 1.2-2.0 equivalents of the compound (3) are added per 1 equivalent of the compound (4) to improve its yield more.
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