CAS: 92122-45-7; Fmoc-D-Lys(Boc)-Oh

该化合物是一种受保护的氨基酸衍生物,广泛用于peptide合成,其主要优势包括与Boc(乙氧-丁基)和Fmoc(9-氟氧基-碳基)组的双重保护,在固相和溶解阶段的peptide化学中能够有选择地制定脱保战略.手工业(R)配置确保合成应用中的立体化学完整性.化合物的叔丁基酯和氟化碳酸化合物保护可提高有机溶性,同时为相继相联步骤提供正交性.其结构特征特别有助于建造具有受控再生选择性的复杂peptide,产品具有高纯度和稳定性,符合严格的研究和药品开发标准.

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上下游产品

CAS号28920-43-6 芴甲氧羰酰氯(Fm°C-Cl) | CAS号31202-69-4 N6-叔丁氧羰基-D-赖氨酸 | CAS号28957-33-7 (R)-3-氨基-2-己内酰胺 | CAS号110990-08-4 Fm°C-D-赖氨酸 | CAS号133083-36-0 N'-叔丁氧羰基-N-芴甲氧羰... | CAS号269061-41-8 Fm°C-D-Lys(Dnp)-OH

合成工艺路线路线简述

  • 92122-45-7 = 92122-45-7
    反应条件:1.1 Reagents: Diisopropylethylamine Solvents: Dichloromethane; 2 H,25 °C1.2 Reagents: Diisopropylethylamine Solvents: Methanol; 0.5 H,25 °C
    标题:Method For Preparing Polypeptide Compound For Pharmaceutical Technology
    参考文献:China]

    = 92122-45-7 [标题:Reaction Conditions
    标题:Preparation Of Amino Acid Derivatives As Hiv Aspartyl Protease Inhibitors
    参考文献:World Intellectual Property Organization]

    = 92122-45-7 [标题:Reaction Conditions
    标题:Propanolamine Derivatives Linked With Bile Acid Used For Treating Disorders Of The Lipid Metabolism
    参考文献:World Intellectual Property Organization]

    31202-69-4 + 82911-69-1 = 92122-45-7
    反应条件:1.1 Reagents: Sodium Bicarbonate Solvents: Tetrahydrofuran; 18 H,Rt
    标题:Selective Targeting Of The Tpx2 Site Of Importin-α Using Fragment-Based Ligand Design
    作者:Holvey,Rhian S.; Valkov,Eugene; Neal,David; Stewart,Murray; Abell,Chris
    参考文献:Chemmedchem 日期:2015 卷标:10(7) 页码:1232-1239]

    28920-43-6 + 2418-95-3 = 92122-45-7
    反应条件:1.1 Reagents: Sodium Bicarbonate Solvents: 1,4-Dioxane,Water1.2 Reagents: Hydrochloric Acid Solvents: Water
    标题:Solution Phase Synthesis Of β-Peptides Using Micro Reactors
    作者:Watts,Paul; Wiles,Charlotte; Haswell,Stephen J.; Pombo-Villar,Esteban
    参考文献:Tetrahedron 日期:2002 卷标:58(27) 页码:5427-5439]

    = 92122-45-7 [标题:Reaction Conditions
    标题:Pharmaceutical Composition Containing Mor Agonist And Kor Agonist,And Uses Thereof
    参考文献:World Intellectual Property Organization]

    = 92122-45-7 [标题:Reaction Conditions
    标题:Preparation Of Amino Acid Derivatives Useful For The Treatment Of Alzheimer'S Disease
    参考文献:World Intellectual Property Organization]

    = 92122-45-7 [标题:Reaction Conditions
    标题:Effective Lowly Cytotoxic Analogs Of An Hiv-Cell Fusion Inhibitor,T22 ([tyr5,12,Lys7]-Polyphemusin Ii)
    作者:Tamamura,Hirokazu; Arakaki,Rieko; Funakoshi,Hanae; Imai,Makoto; Otaka,Akira; Et Al
    参考文献:Bioorganic & Medicinal Chemistry 日期:1998 卷标:6(2) 页码:231-238]

    205812-10-8 = 92122-45-7 + 71989-26-9 [标题:Reaction Conditions
    标题:A New Single-Urea-Bound 3,5-Dimethylphenylcarbamoylated β-Cyclodextrin Chiral Stationary Phase And Its Enhanced Separation Performance In Normal-Phase Liquid Chromatography
    作者:Lin,Chun; Fan,Jun; Liu,Wenna; Chen,Xiaodong; Ruan,Lijun; Et Al
    参考文献:Electrophoresis 日期:2018 卷标:39(2) 页码:348-355
📜N6-叔丁氧羰基-D-赖氨酸,9-芴甲基-N-琥珀酰亚胺基碳酸酯置于碳酸氢钠体系中,用 四氢呋喃 作为反应溶剂,化学反应 18.0H,以97%的收率获得产物n-Alpha-芴甲氧羰基-N-Epsilon-叔丁氧羰基-D-赖氨酸
参考文献:使用基于片段的配体设计选择性靶向 Importin-α 的 Tpx2 位点
标题:使用基于片段的配体设计选择性靶向 Importin-α 的 Tpx2 位点
摘要:蛋白质-蛋白质相互作用是困难的治疗靶点,在不破坏其他重要相互作用的情况下抑制病理相关相互作用提出了额外的挑战.在此,我们报告了潜在的抗癌靶点 Tpx2-Importin-α 相互作用如何实现这一目标.importin-α 是一种核转运蛋白,可调节纺锤体组装蛋白 Tpx2.它有两个结合位点--主要和次要--与合作伙伴结合.大多数核运输货物使用主要站点,而 Tpx2 主要绑定到次要站点.基于片段的方法被用于识别结合 Importin-α 的小分子,晶体学研究确定了一个铅系列,观测到该铅系列与次要位点特异性结合,代表了该位点特异性的第一个配体.结构指导的合成为这些片段的精细化提供了信息,以探索次要位点和主要位点之间配体选择性的来源.这些配体是开发这种蛋白质-蛋白质相互作用抑制剂的起点.
DOI:10.1002/cmdc.201500014

海关参考信息

专利信息


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:US-2024209034-A1
优先权日:2021-04-12
标题:Engineering peptides for a a vb6 integrin binding and related methods of use and synthesis
发明人：SELLERS DREW; CARDLE IAN; PUN SUZIE HWANG
权利人:UNIV WASHINGTON; SEATTLE CHILDRENS HOSPITAL D/B/A SEATTLE CHILDRENS RES INSTITUTE
摘要:Embodiments of the claimed invention are directed to synthetic peptides comprising an amino acid sequence of X 1 X 2 VX 3 NLRGDLQVLX 4 QKVCX 5 T (SEQ ID NO:18), wherein at least one of X 1 and X 2 is a cysteine, and wherein one or more of X 3 , X 4 , and X 5 is a non-natural amino acid. Also described are methods of using the claimed embodiments for inhibiting growth of a cancer cell overexpressing integrin αvβ6. Additionally, also described are methods of using the claimed embodiments for detecting a cancer cell overexpressing integrin αvβ6.

专利号:CN-107056894-B
优先权日:2017-05-26
标 题:A kind of method for fragment method solid-phase synthesis of ganirelix acetate

专利号:US-2022185846-A1
优先权日:2019-03-28
标 题:Methods for synthesizing beta-homoamino acids
发明人：MANTHATI SURESH KUMAR; BHANDARI ASHOK; MASJEDIZADEH MOHAMMAD REZA
权利人:PROTAGONIST THERAPEUTICS INC
摘要:Methods of making β-homoamino acids as intermediate for synthesis of peptide monmer and dimer α4β7-antagonists are disclosed. The disclosed methods include solid phase and solution phase methods.

专利号:WO-2010081882-A2
优先权日:2009-01-16
标 题 :Synthesis of new protected azahistidines, their processes and their use in synthesises

专利号:CN-115925790-A
优先权日:2016-03-23
标 题:Method for the synthesis of α4β7 peptide antagonists

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合成参考文献


摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025).
摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025).
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