CAS: 82317-83-7; (R)-2-((Tert-Butoxycarbonyl)Amino)-3-(4-(Trifluoromethyl)Phenyl)Propanoic Acid

该化合物是一种受保护的氨基酸衍生物,其成分为一个Boc(乙氧碳基)组和苯环上的三氟甲基替代物,该化合物广泛用于peptide合成,特别是在需要纳入氟芳香侧链的情况下.Boc组在基本条件下提供稳定性,可以在酸性条件下有选择地予以保护,促进受控的peptide延长.三氟甲基组增强脂质和代谢稳定性,使其在药用化学中具有价值,用于设计生物活性聚醚和小分子.其高纯度和定义明确的立体化学确保了合成应用的可靠性能.

结构式图片

相似化合物

114873-07-3 114926-38-4 238742-88-6

上下游产品

CAS号24424-99-5 二碳酸二叔丁酯 | CAS号1082750-11-5 (R)-2-acetamido... | CAS号82337-58-4 AC-DL-PHE(4-CF3)-OH | CAS号82317-73-5 methyl 2-acetam... | CAS号82317-77-9 methyl (R)-2-ac... | CAS号269726-77-4 (R)-3-((叔丁氧羰基)氨...

合成工艺路线路线简述

  • 176795-01-0 = 82317-83-7
    反应条件:1.1 Reagents: Lithium Hydroxide Solvents: Methanol,Tetrahydrofuran,Water; 6 H,0 °C
    标题:Discovery Of Pyrrolopyrimidine Inhibitors Of Akt
    作者:Blake,James F.; Et Al
    参考文献:Bioorganic & Medicinal Chemistry Letters 日期:2010 卷标:20(19) 页码:5607-5612]

    455-19-6 + 89524-98-1 = 82317-83-7
    反应条件:1.1 Reagents: 1,1,3,3-Tetramethylguanidine Solvents: Dichloromethane; 2 H,0 °C -> Rt2.1 Reagents: Hydrogen Catalysts: (1,2-Bis((R,R)-2,5-Diethyl-1-Phospholidinyl)Benzene)(1,5-Cyclooctadiene)Rhodium(... Solvents: Methanol,Ethyl Acetate; 12 H,40 Psi,Rt3.1 Reagents: Lithium Hydroxide Solvents: Methanol,Tetrahydrofuran,Water; 6 H,0 °C
    标题:Discovery Of Pyrrolopyrimidine Inhibitors Of Akt
    作者:Blake,James F.; Et Al
    参考文献:Bioorganic & Medicinal Chemistry Letters 日期:2010 卷标:20(19) 页码:5607-5612]

    24424-99-5 + 114872-99-0 = 82317-83-7
    反应条件:1.1 Reagents: Sodium Hydroxide Solvents: 1,4-Dioxane,Water; 20 H,Rt1.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 2 - 4,Rt
    标题:Structure-Activity Relationship Studies On (R)-Pfi-2 Analogues As Inhibitors Of Histone Lysine Methyltransferase Setd7
    作者:Lenstra,Danny C.; Et Al
    参考文献:Chemmedchem 日期:2018 卷标:13(14) 页码:1405-1413]

    = 82317-83-7
    反应条件:1.1 Reagents: Hydrogen Catalysts: (1,2-Bis((R,R)-2,5-Diethyl-1-Phospholidinyl)Benzene)(1,5-Cyclooctadiene)Rhodium(... Solvents: Methanol,Ethyl Acetate; 12 H,40 Psi,Rt2.1 Reagents: Lithium Hydroxide Solvents: Methanol,Tetrahydrofuran,Water; 6 H,0 °C
    标题:Discovery Of Pyrrolopyrimidine Inhibitors Of Akt
    作者:Blake,James F.; Et Al
    参考文献:Bioorganic & Medicinal Chemistry Letters 日期:2010 卷标:20(19) 页码:5607-5612
📜Diethyl 2-Acetamido-2-<<4-(Trifluoromethyl)Phenyl>Methyl>Malonate置于盐酸,Sodium Hydroxide,三氟化硼乙醚,Magnesium Oxide体系中,用 1,4-二氧六环 作为反应溶剂,化学反应 3.0H,反应生成 Boc-D-4-三氟甲基苯丙氨酸
参考文献:Synthesis And Biological Activity Of Some Very Hydrophobic Superagonist Analogs Of Luteinizing Hormone-Releasing Hormone
标题:Synthesis And Biological Activity Of Some Very Hydrophobic Superagonist Analogs Of Luteinizing Hormone-Releasing Hormone
摘要:The Effect Of Increased Hydrophobicity At Position 6 Of Luteinizing Hormone-Releasing Hormone (Lh-Rh) Has Been Investigated By The Incorporation Of A Series Of 15 Very Hydrophobic,Unnatural D-Amino Acids At This Position. The Unnatural Amino Acids Studied Can Be Considered Analogues Of Phenylalanine With Carbocyclic Aromatic Side Chains Consisting Of Substituted Phenyl (E.G.,2,4,6-Trimethylphenyl,P-Biphenyl) Or Polycyclic Aromatic (E.G.,Naphthalene,Anthracene) Units. When Enzymatic Resolution (Subtilisin Carlsberg) Of The Most Hydrophobic Amino Acids Failed,The Racemic Amino Acids Were Incorporated,And The Diastereomeric Lh-Rh Analogues Were Resolved By Preparative High-Performance Liquid Chromatography. The Analogues Were Synthesized By The Solid-Phase Technique. All Of The Synthetic Compounds Were Very Potent Lh-Rh Superagonists,But [6-(3-(2-Naphthyl)-D-Alanine)]Lh-Rh,[6-(3-(2-Naphthyl)-D-Alanine),7-(N Alpha-Methylleucine)]Lh-Rh And [6-(3-(2,4,6-Trimethylphenyl)-D-Alanine)]Lh-Rh Appear To Be Among The Most Potent Lh-Rh Agonist Analogues Yet Reported When Tested In A Rat Estrus Cyclicity Suppression Assay Designed To Show The Paradoxical Antifertility Effects Of These Compounds [ed50 Approximately 7 X 10(-8) G; Twice Daily In Saline]. These Analogues Are Twice As Potent As [d-Trp6,Pronhet9]Lh-Rh In This Assay System (I.E.,Approximately 200 Times The Potency Of Lh-Rh).
DOI:10.1021/jm00349A006

海关参考信息

专利信息


专利号:US-8933018-B2
优先权日:2011-02-07
标题 :Boron containing polybasic bacterial efflux pump inhibitors and therapeutic uses thereof
发明人:GLINKA TOMASZ; HIGUCHI ROBERT; HECKER SCOTT; EASTMAN BRIAN; RODNY OLGA
权利人:GLINKA TOMASZ; HIGUCHI ROBERT; HECKER SCOTT; EASTMAN BRIAN; RODNY OLGA; REMPEX PHARMACEUTICALS INC
摘要:Disclosed herein are polybasic bacterial efflux pump inhibitors containing boronic acid functionality and their methods of synthesis, methods of use, and pharmaceutical compositions. Some embodiments include methods of treating or preventing a bacterial infection by co-administering to a subject infected with bacteria or at risk of infection with bacteria the efflux pump inhibitor with another anti-bacterial agent.

供应商参考报价(招募中)

品牌试剂参考报价(招募中)

📌 第三方产品分析报告

✅ COA系统入驻 | 共享模式

合成参考文献


参考文献:10.1007/s00894-018-3593-z
摘要:Kapusta K, Sizochenko N, Karabulut S, Okovytyy S, Voronkov E, Leszczynski J. QSPR modeling of optical rotation of amino acids using specific quantum chemical descriptors. Journal of Molecular Modeling. 2018 Feb 17;24(3):59. doi: 10.1007/s00894-018-3593-z.
📝 需求与反馈
尽可能描述清楚需求与问题信息
×

通知