首页> 外国专利> 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

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

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.
机译:目的:提供一种高产率地制备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,该方法可用作治疗所获得的化合物的中间体。免疫缺陷综合症(艾滋病)。组成:制备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的特征在于下一步:使5-(羟基保护的)-5-(在碱和极性或非极性有机溶剂存在下于0-150℃,优选25-90℃存在下,将式(4)取代或未取代的)式(4)的2-脱氧尿苷与式(3)的1,1-磺酰二咪唑。C。任选地,每1当量的化合物(4)添加1.2-2.0当量的化合物(3),以进一步提高其产率。

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