CAS: 752174-62-2; Ethyl (2R,4S)-4-Amino-5-{[1,1'-Biphenyl]-4-Yl}-2-Methylpentanoate

该化合物是具有特定立体化学特征的手性化合物,其配置(2R,4S)表明,该化合物具有乙基酯功能组,有助于其溶解性和再活性;双联苯混合物的存在增强了其疏水特性,有可能影响其生物活动和相互作用;氨基结构中的氨基组表示,它可能参与氢联结,从而影响其药理基因特性;此外,分形烷基链(2-甲基苯甲酸盐)具有阻碍性,可能会影响其相容灵活性;

结构式图片

MSDS等安全信息

    上下游产品

    (2R,4S)-5-([1,1'-Biphenyl]-4-yl)-4-Amino-2-Methylpentanoic Acid 1039307-95-3
    Phenyl (2R,4S)-5-([1,1'-Biphenyl]-4-yl)-4-Amino-2-Methylpentanoate
    (2R,4S)-乙基 5-([1,1'-联苯]-4-基)-4-((叔丁氧羰基)氨基)-2-甲基戊酸 Ethyl (2R,4S)-5-([1,1'-Biphenyl]-4-yl)-4-((Tert-Butoxycarbonyl)Amino)-2-Methylpentanoate 149709-60-4
    (2R,4S)-5-(联苯-4-基)-4-[(叔丁氧基羰基)氨基]-2-甲基戊酸 (2R,4S)-5-(Biphenyl-4-yl)-4-[(Tert-Butoxycarbonyl)Amino]-2-Methylpentanoic Acid 1012341-50-2

    合成工艺路线路线简述

      4-联苯乙酸置于盐酸,甲醇,4-二甲氨基吡啶,丙二酸环(亚)异丙酯,氯化亚砜,磷酸吡哆醛,三甲基乙酰氯,Sodium Hydride,异丙胺,N,N-二异丙基乙胺,三氟乙酸,Sodium Hydroxide体系中,用 四氢呋喃,二氯甲烷,水,二甲基亚砜 作为反应溶剂,化学反应 87.0H,反应生成 (2R,4S)-乙基 5-([1,1'-联苯]-4-基)-4-氨基-2-甲基戊酸
      参考文献:Sacubitril Intermediate And Preparation Method Thereof
      标题:Sacubitril Intermediate And Preparation Method Thereof
      摘要:本发明涉及一种萨库比曲中间体及其制备方法.本文披露的萨库比曲中间体可通过一种化合物的去保护反应制备.此外,该中间体可用作合成萨库比曲的原料.本文披露的方法具有易获得的原料,简单的制备过程,低成本,环保等优点,非常适合工业生产.

      海关参考信息

      专利信息


      专利号:WO-2017033128-A1
      优先权日:2015-08-25
      标题 :Biphenyl-substitued 4-amino-butyric acid derivatives and their use in the synthesis of nep inhibitors
      发明人:HOOK DAVID; KU JIE; ZHOU JIANGUANG
      权利人:NOVARTIS AG; HOOK DAVID; KU JIE; ZHOU JIANGUANG
      摘要:The invention relates to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, in particular neutral endopeptidase (NEP) inhibitors and prodrugs thereof.

      专利号:WO-2017051326-A1
      优先权日:2015-09-23
      标 题 :New processes and intermediates useful in synthesis of nep inhibitors
      发明人:MARTIN BENJAMIN; PENN GERHARD; SCHENKEL BERTHOLD; BOURNE SAMUEL; LAU SHING-HING; LEY Steven
      权利人:NOVARTIS AG; MARTIN BENJAMIN; PENN GERHARD; SCHENKEL BERTHOLD; BOURNE SAMUEL; LAU SHING-HING; LEY Steven
      摘要:The invention relates to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, in particular neutral endopeptidase (NEP) inhibitors such as sacubitril, and prodrugs thereof.

      专利号:US-10851059-B2
      优先权日:2016-08-17
      标题:Processes and intermediates for NEP inhibitor synthesis
      发明人:KLEINBECK-RINIKER FLORIAN KARL; MAFLI IVES; MARTIN BENJAMIN; PENN GERHARD; SEDELMEIER GOTTFRIED; SEDELMEIER JOERG; VENTURONI FRANCESCO
      权利人:NOVARTIS AG
      摘要:The present invention relates to a new chemical synthesis, intermediates and catalysts useful for the preparation of the neprilysin (NEP) inhibitor sacubitril, inter alia via nitro 5 compounds. It further relates to new intermediate compounds and their use for said new chemical synthesis route, as well as a new catalyst ligand.

      专利号:CN-118109528-A
      优先权日:2024-04-10
      标题 :A method for biocatalytic synthesis of sacubitril intermediate (2R, 4S)-5-([1,1'-biphenyl]-4-yl)-4-amino-2-methylvaleric acid

      专利号:CN-118516422-A
      优先权日:2024-04-10
      标 题:A method for biocatalytic synthesis of sacubitril intermediates

      专利号:US-11434192-B2
      优先权日:2015-12-10
      标 题:Process and intermediates
      发明人:KLEINBECK-RINIKER FLORIAN KARL; MARTIN BENJAMIN; PENN GERHARD; VENTURONI FRANCESCO; SCHLAMA THIERRY; RUCH THOMAS; ALLMENDINGER THOMAS; WIETFELD BERNHARD; FILIPPONI PAOLO
      权利人:NOVARTIS AG
      摘要:The present invention relates to a new chemical synthesis, intermediates and catalysts useful for the preparation of the neprilysin (NEP) inhibitor sacubitril. It further relates to new intermediate compounds and their use for said new chemical synthesis route.
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      合成参考文献


      参考文献:10.1055/s-0040-1707096
      摘要:Synthesis of Sacubitril. Synfacts. 2020 Jul 21;16(08):0877. doi: 10.1055/s-0040-1707096.
      参考文献:10.1055/s-0035-1561109
      摘要:Synthesis of Sacubitril. Synfacts. 2016 Jan 19;12(02):0110. doi: 10.1055/s-0035-1561109.
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