CAS: 205445-51-8; Boc-D-Phe(3,4-Dif)-Oh

该化合物是苯丙胺的氟化衍生物,其特点是对氨基环的3,4个位置的氨基组和二氟化物的Boc(乙氧碳基)保护,该化合物广泛用于peptide合成,特别是用于引入氟化芳香侧链,这可以增强代谢稳定性,改变疏水性,并改进生物活性peptids的结合性.Boc组确保在温酸条件下有选择地减少保护,促进逐步固相或溶相合成.氟原子的存在具有独特的电子和消毒特性,对结构-活动关系(SAR)研究和药物研究十分宝贵.高纯度和一贯性对于合成应用的可靠性能至关重要.

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相似化合物

198474-90-7 198560-43-9 31105-90-5

上下游产品

tert-butyl dicarbonatedi-tert-butyl dicarbonate (L)-2-amino-3-(3,4-difluorophenyl)propanoic acid 2-Acetylamino-2-(3,4-difluorobenzyl)malonic acid diethyl ester alpha-bromo-3,4-difluorotoluene(4aS,8aR)-2-{1-[(2R)-2-amino-3-(3,4-difluorophenyl)propanoyl]piperidin-4-yl}-4-(3,4-dimethoxyphenyl)-4a,5,6,7,8,8a-hexahydrophthalazin-1(2H)-one hydr°Chloride tert-butyl [(2R)-3-(3,4-difluorophenyl)-1-{4-[(4aS,8aR)-4-(3,4-dimethoxyphenyl)-1-oxo-4a,5,6,7,8,8a-hexahydrophthalazin-2(1H)-yl]piperidin-1-yl}-1-oxopropan-2-yl]carbamate (R)-1-methyl-pyrrolidine-2-carboxylic acid [(S)-1-[(6-amino-pyridin-3-ylmethyl)-carbamoyl]-2-(3,4-difluoro-phenyl)-ethyl]-amide 3-methyl-1H-pyrrole-2-carboxylic acid [(S)-1-[(6-amino-pyridin-3-ylmethyl)-carbamoyl]-2-(3,4-difluoro-phenyl)-ethyl]-amide trifluoroacetate

合成工艺路线路线简述

    📜Methyl (2R)-2-{[(Tert-Butoxy)Carbonyl]Amino}-3-(3,4-Difluorophenyl)Propanoate置于水,Lithium Hydroxide体系中,用 四氢呋喃,甲醇 用作溶剂,化学反应 6.0H,反应生成Boc-D-3,4-二氟苯丙氨酸
    参考文献:Discovery Of Pyrrolopyrimidine Inhibitors Of Akt
    标题:Discovery Of Pyrrolopyrimidine Inhibitors Of Akt
    摘要:The Discovery And Optimization Of A Series Of Pyrrolopyrimidine Based Protein Kinase B (Pkb/akt) Inhibitors Discovered Via Hts And Structure Based Drug Design Is Reported. The Compounds Demonstrate Potent Inhibition Of All Three Akt Isoforms And Knockdown Of Phospho-Pras40 Levels In Lncap Cells And Tumor Xenografts. (C) 2010 Elsevier Ltd. All Rights Reserved.
    Doi:10.1016/j.Bmcl.2010.08.053

    海关参考信息

    专利信息


    专利号:US-6514997-B2
    优先权日:1999-12-03
    标题:Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis
    发明人:DRAGOVICH PETER S; PRINS THOMAS J; ZHOU RU; JOHNNSON JR THEODORE O
    权利人:AGOURON PHARMA
    摘要:Compounds of the formula: n where the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the picornaviral 3C protease. Also disclosed are compounds of the formula: n where the formula variables are as defined herein that advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as rhinovirus 3C proteases. Intermediates and synthetic methods for preparing such compounds are also described.

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    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献

    [参考文献]: Luckose F, Et Al. Effects Of Amino Acid Derivatives On Physical, Mental, And Physiological Activities. Crit Rev Food Sci Nutr. 2015;55(13):1793-949.

    合成参考文献

    合成方法参考DOI号:10.1016/S0040-4039(99)02191-7
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