CAS: 66845-42-9; Z-D-Lys(Boc)-Oh

该化合物是一种受保护的氨基酸碱,对蛋白合成至关重要.该化合物有两种保护性组:苯氧基碳基(Z)组和乙-丁-丁碳基(Boc)组,用于防止在浸泡合成过程中的不必要反应.这些保护性组的存在加强了赖氨基侧链的稳定性,同时允许在合成的特定阶段有选择地取消保护.该化合物一般是白色的对非白固态,溶于二氯甲烷和二甲基芳基胺等有机溶剂中,但在水中溶解较少.其分子结构包括一个主要的安咪非氨基化学和药物的精密性控制领域.

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10009-20-8 105047-45-8 106719-44-2

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CAS号24424-99-5 二碳酸二叔丁酯 | CAS号70671-54-4 Cbz-D-赖氨酸

合成工艺路线路线简述

    📜二碳酸二叔丁酯,Cbz-D-赖氨酸置于sodium Hydroxide体系中,用 甲醇 作为反应溶剂,化学反应 10.0H,反应生成 N-苄氧羰基-N'-叔丁氧羰基-L-赖氨酸
    参考文献:放松抗体催化反应中的底物特异性:N-Cbz-氨基酸酯的对映选择性水解
    标题:放松抗体催化反应中的底物特异性:N-Cbz-氨基酸酯的对映选择性水解
    摘要:对于通常用于有机合成化学的催化抗体,它必须能够接受广泛的底物,同时保持高选择性.在这项工作中,我们提出了一种半抗原设计,使抗体催化剂具有两种相反的特性,例如高对映选择性和广泛的底物特异性.外消旋半抗原 2 诱导两类不同的催化抗体水解 N-Cbz-氨基酸酯 1 的 L-或 D-异构体. 在外消旋酯 9 的动力学拆分中,抗体 7G12 和 3G2 产生 96% 的 L-Ee D-10 的 Ee 分别为 10% 和 94%.此外,抗体 7G12 显示出广泛的底物特异性,可水解 Ala (1A),Leu (1B),Norleu (1C),Met (1D),Phe (1E),Val (1F) 和苯基甘氨酸 (1G) 的 L-酯) 具有高对映选择性.抗体 3G2 还水解了这些酯的 D-异构体而不牺牲对映选择性.这一观察结果表明,使用与抗原结合位点紧密贴合的半抗原,并在...
    DOI:10.1021/ja952220W

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    专利信息


    专利号:EP-0406931-B1
    优先权日:1989-06-30
    标 题 :New analogues of all-bond retroinverted thymopentin, the method for the synthesis of the same and their employment for the preparation of pharmaceutical compositions
    发明人：MARIOTTI SABINA; SISTO ALESSANDRO; NENCIONI LUCIANO; VILLA LUIGI; PESSI ANTONELLO
    权利人:SCLAVO SPA
    摘要:New thymopentin (TP5) analogues whose bonds in the peptide chain are all retro-inverted are disclosed. Such new compounds have the following general formula (I) wherein R is hydrogen or an acyl radical, and R<1> is a group of the formula -OR<2>, wherein R<2> is a hydrogen atom or a hydrocarbon radical, and the corresponding basic or acid addition salts which are pharmaceutically acceptable. The new compounds have immunostimulating activity.

    专利号:US-10407468-B2
    优先权日:2016-03-23
    标 题 :Methods for synthesizing α4β7 peptide antagonists
    发明人：BHANDARI ASHOK; MANTHATI SURESH KUMAR; MEHROTRA MUKUND M; ANANDAN SAMPATH-KUMAR; PATEL DINESH V
    权利人:PROTAGONIST THERAPEUTICS INC
    摘要:The present invention provides methods of making α4β7 peptide monomer and dimer antagonists. Methods of the present invention include solid phase and solution phase methods, as well as synthesis via condensation of smaller peptide fragments. Methods of the present invention further include methods directed to the synthesis of peptides comprising one or more penicillamine residues.

    专利号:EP-0406931-A2
    优先权日:1989-06-30
    标题 :New analogues of all-bond retroinverted thymopentin, the method for the synthesis of the same and their employment for the preparation of pharmaceutical compositions

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    主要参考文献

    参考标题:Facile N-Urethane-Protected α-Amino/peptide Thioacid Preparation Using Edc And Na2S
    作者:Vommina Sureshbabu,T. Vishwanatha,M. Samarasimhareddy |发布日期:2012.1
    摘要:We Report Herein An Efficient Protocol For The Synthesis Of N-Urethane-Protected î+/--Amino/peptide Thioacids From Their Corresponding Acids Mediated By Edc And Na2S. The Fast Reaction Under Mild Conditions Enabled The Process To Be Completed In Shorter Duration With Good Yield Circumventing Column Purification. The Chemistry Is Compatible With A Wide Variety Of Urethane Protecting Groups, Side-Chain Functionalities, And Sterically Hindered Amino Acids.

    合成参考文献


    参考文献:10.1007/s11094-018-1885-3
    摘要:Sazonova NM, Tarasyuk AV, Shumskii AN, Rebeko AG, Antipov PI, Logvinov IO, Antipova TA, Gudasheva TA. Synthesis and In Vitro Neuroprotector Activity of Diastereoisomers of a Dimeric Dipeptide Mimetic of Nerve Growth Factor GK-2. Pharmaceutical Chemistry Journal. 2018 Nov 09;52(8):704–10. doi: 10.1007/s11094-018-1885-3.
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