CAS: 1355049-94-3; (3R,4R,5R)-2-(4-Aminopyrrolo[2,1-F][1,2,4]Triazin-7-yl)-3,4-Bis(Benzyloxy)-5-((Benzyloxy)Methyl)Tetrahydrofuran-2-Ol

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1355357-49-1 1191237-69-0 1191237-80-5

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7-bromo-pyrrolo[2,1-f][1,2,4]triazin-4-ylamine (3R,4R,5R)-3,4-Bis-benzyloxy-5-benzyloxymethyl-dihydro-furan-2-one 2,3,5-tri-O-benzyl-D-ribofuranose 7-iodopyrrolo-[2,1-f][1,2,4]-triazin-4-amine 7-((2S,3S,4R,5R)-3,4-bis(benzyloxy)-5-((benzyloxy)methyl)-tetrahydrofuran-2-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (2R,3R,4R,5R)‐2‐{4‐aminopyrrolo[2,1‐f][1,2,4]triazin‐7‐yl}‐3,4‐bis(benzyloxy)‐5‐[(benzyloxy)methyl]tetrahydrofuran‐2‐carbonitrile (2S,3R,4R,5R)-2-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-3,4-bis(benzyloxy)-5-((benzyloxy)methyl)tetrahydrofuran-2-carbonitrile

合成工艺路线路线简述

    📜D-(+)-核糖酸-1,4-内酯置于正丁基锂,三氟甲磺酸体系中,用 四氢呋喃,1,4-二氧六环,正己烷 用作溶剂,化学反应 6.0H,反应生成瑞德西韦杂质1
    参考文献:带有核糖,2'-脱氧核糖和2',3'-脱氧核糖糖基的吡咯并[2,1-F] [1,2,4]三嗪c-核苷的合成及生物评价
    标题:带有核糖,2'-脱氧核糖和2',3'-脱氧核糖糖基的吡咯并[2,1-F] [1,2,4]三嗪c-核苷的合成及生物评价
    摘要:描述了迄今未知的吡咯并[2,1-F ] [1,2,4]三嗪c-核苷的合成.在4-Aza-7,9-Dideazaadenine的7位引入了结构变异(氯,溴,碘和氰基).另外,带有2'-脱氧,2',3'-二脱氧和2',3'-脱氢二脱氧核糖的吡咯并[2,1-F ] [1,2,4]三嗪c-核苷也是准备好了.在这些类似物中,吡咯并[2,1-F ] [1,2,4]三嗪c-核糖核苷在核碱基7位具有氢原子或氰基,在多种癌细胞系中均显示出强力的细胞毒活性. .
    Doi:10.1002/cmdc.201700657

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    专利信息


    专利号:US-11612614-B2
    优先权日:2020-10-20
    标题:Isomorphs of Remdesivir and methods for synthesis of same
    发明人：TRIPATHI VINAY SHANKAR; PATEL AKSHAY NIKHIL
    权利人:ANZALP PHARMASOLUTIONS PVT LTD
    摘要:A new isoform of 2-ethylbutyl (2S)-2-[[[(2R,3S,4R,5R)-5-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-5-cyano-3/4-dihydroxyoxolan-2-yl]methoxy-phenoxyphosphoryl]amino]propanoate (Remdesivir) having increased water solubility is disclosed, along with methods for making the same. Also disclosed are solid and liquid pharmaceutical compositions suitable for treating viral infections such as Arenaviridae, Coronaviridae, Filoviridae, Flaviviridae, or Paramyxoviridae viral infections which contain an effective amount of Remdesivir prepared according to the inventive method and the use of those compositions for treating such viral infections.

    专利号:US-2021228605-A1
    优先权日:2020-10-20
    标题:Isomorphs of remdesivir and methods for synthesis of same

    专利号:US-2021161927-A1
    优先权日:2020-10-20
    标 题:Isomorphs of remdesivir and methods for synthesis of same

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    合成参考文献


    摘要:Kleemann, A.; Engel, J.; Kutscher, B.; Reichert, D., Pharmaceutical Substances[Online], Thieme: Stuttgart, (2020)
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