CAS: 1157884-58-6; Sofosbuvir Impurity 32

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874638-80-9 879551-04-9 1946820-91-2

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    (2R,3R,4R)-2-[(苯甲酰氧基)甲基]-4-羟基-4-甲基-5-氧代氧杂环戊-3-基苯甲酸酯 3,5-Di-O-Benzoyl-2-C-Methyl-D-Ribono-γ-Lactone 729596-46-7

    合成工艺路线路线简述

      📜2-C-甲基-D-核糖酸-1,4-内酯置于吡啶,四丁基氟化铵,三乙胺体系中,用 二氯甲烷,乙酸乙酯,丙酮 用作溶剂,化学反应 2.08H,反应生成(2S)-3,5-二-O-苯甲酰基-2-氟-2-C-甲基-D-核糖酸-C-内酯
      参考文献:邻近团体的参与策略:轻松合成3,5-二-O-苯甲酰基-2-C-甲基-D-阿拉伯糖基-γ-内酯
      标题:邻近团体的参与策略:轻松合成3,5-二-O-苯甲酰基-2-C-甲基-D-阿拉伯糖基-γ-内酯
      摘要:为3,5-二-合成的简单且有效的方法ö-苯甲酰基-2-ç甲基d报道通过邻基参与机制-Arabino-γ内酯.该化合物可能是合成核苷抗病毒剂的有用前体.
      Doi:10.1016/j.Tetlet.2015.05.085

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      专利信息


      专利号:US-9376410-B2
      优先权日:2012-10-10
      标题 :(2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone and preparation method and use thereof
      发明人:WANG GUAN; JIANG XIANGRUI; GONG XUDONG; CHEN WEIMING; ZHU FUQIANG; ZHANG RONGXIA; ZHAO XIANGUO
      权利人:TOPHARMAN SHANGHAI CO LTD; SHANGHAI INST MATERIA MEDICA; TOPHARMAN SHANDONG CO LTD; SHANGHAI INST MATERIA MEDICA
      摘要:This invention disclose (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone in a single configuration and preparation method and use thereof. The (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone, or a pharmaceutically acceptable salt, an ester, a prodrug or a solvate thereof according to the invention are important intermediates of a variety of anti-viral and anti-tumor active ingredients. A compound obtained from (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone via an acylation reaction can be directly used for preparing various anti-viral and anti-tumor drugs. The Chiral synthesis method and the spontaneous resolution method of the compound of (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone according to the invention have the following advantages: the reaction routes are short and simple with high yield and low cost, which are suitable for industrial application.

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      合成参考文献

      参考DOI号:10.1016/j.tetlet.2015.05.085
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