公开(公告)号：KR1020010056060A

公开(公告)日：2001-07-04

申请号：KR1019990057477

申请日：1999-12-14

Applicant: 한국화학연구원

Inventor： 노재성 ,  신동성 ,  안미자

IPC: C07D498/12

Abstract: 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.

Abstract translation: 目的：提供以高产率制备5-（羟基保护的）-5-（取代或未取代）2,3-脱水-2-脱氧尿苷化合物的方法，其可用作用于治疗所获得的化合物的中间体 免疫缺陷综合征（AIDS）。 构成：5-（羟基保护）-5-（取代或未取代）2,3-脱水-2-脱氧尿苷化合物的制备方法的特征在于下列步骤：使5-（羟基保护的）-5-（ 取代或未取代的）式（4）的脱氧尿苷与式（3）的1,1-磺酰基二咪唑在碱和极性或非极性有机溶剂存在下在0-150℃，优选25-90度 。C。 任选地，每1当量化合物（4）加入1.2-2.0当量的化合物（3），以提高其产率。