CAS: 54594-06-8; H-D-Gly(Allyl)-Oh

该化合物是一种氨酸衍生物,其特点是存在附于甘蓝脊柱的Allyls组,其分子结构具有简单的氨基组(-NH2),一个碳球酸组(-COOH)和一个 allyl侧链,有助于其独特的再活动性和特性.该化合物已知是某些酶的抑制剂,特别是那些参与...

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合成工艺路线路线简述

    📜(2R,Rs)-2-(Tert-Butylsulfinamido)Pent-4-Enoic Acid置于盐酸体系中,用 水 作为反应溶剂,化学反应 4.0H,以69%的收率获得产物d-烯丙基甘氨酸
    参考文献:Diastereoselective Amidoallylation Of Glyoxylic Acid With Chiral Tert-Butanesulfinamide And Allylboronic Acid Pinacol Esters: Efficient Synthesis Of Optically Active γ,δ-Unsaturated α-Amino Acids
    标题:Diastereoselective Amidoallylation Of Glyoxylic Acid With Chiral Tert-Butanesulfinamide And Allylboronic Acid Pinacol Esters: Efficient Synthesis Of Optically Active γ,δ-Unsaturated α-Amino Acids
    摘要:A Convenient Synthesis Of Delta,Gamma-Unsaturated Amino Acids Has Been Developed. After A Mixture Of (R)-Tert-Butanesulfinamide And Glyoxylic Acid With Molecular Sieves In Ch2Cl2 Was Stirred For 42 H At Room Temperature,Allylboronic Acid Pinacol Ester Was Added To The Mixture To Give (R)-2-((R)-Tert-Butanesulfinamido)Pent-4-Enoic Acid With High Diastereoselectivity. The Corresponding Reaction Of (Z)-Crotylboronic Acid Pinacol Ester Produced No Product; However,That Of (E)-Crotylboronic Acid Pinacol Ester Produced (2R,3S)-2-((R)-Tert-Butylsulfinamido)-3-Methylpent-4-Enoic Acid With Excellent Diastereoselectivity. (C) 2013 Elsevier Ltd. All Rights Reserved.
    DOI:10.1016/j.Tetasy.2013.07.026

    海关参考信息

    专利信息


    专利号:US-2012282180-A1
    优先权日:2011-05-06
    标题 :Compounds with Matrix-Metalloproteinase Inhibitory Activity and Imaging Agents Thereof
    发明人:KOLB HARTMUTH C; HAUFE GUENTER; BEHRENDS MALTE; KOPKA KLAUS; WAGNER STEFAN; HUGENBERG VERENA; BREYHOLZ HANS-JOERG; HERMANN SVEN; SCHAEFERS MICHAEL
    权利人:KOLB HARTMUTH C; HAUFE GUENTER; BEHRENDS MALTE; KOPKA KLAUS; WAGNER STEFAN; HUGENBERG VERENA; BREYHOLZ HANS-JOERG; HERMANN SVEN; SCHAEFERS MICHAEL
    摘要:The present invention relates to the field of therapeutic and diagnostic agents and more specifically to compounds of formula (I) that are inhibitors of matrix-metalloproteinases (MMPs) and are useful in the treatment of diseases related thereto such as cardiovascular diseases, inflammatory diseases and malignant diseases. One embodiment of the invention is a compound of formula (I) labeled with a 18-fluorine atom having matrix metalloproteinase inhibitory activity suitable for diagnostic imaging. Also disclosed in the present invention is a pharmaceutical composition comprising the inhibitors of matrix-metalloproteinases (MMPs) of the invention or the corresponding labeled compounds useful as diagnostic imaging agents of the invention in a form suitable for mammalian administration. The invention furthermore discloses intermediates in the synthesis of the inhibitors of matrix-metalloproteinases (MMPs) of the invention and of the diagnostic imaging agents of the invention and kits for the preparation of the pharmaceutical composition of the invention.

    专利号:US-12234299-B2
    优先权日:2018-11-22
    标 题 :Peptides for inducing bacteriocin synthesis and methods to identify and/or select and/or optimize the same
    发明人:MIGNOLET JOHANN; HOLS PASCAL; LEDESMA GARCÃ?A LAURA
    权利人:SYNGULON S A; UNIV CATHOLIQUE LOUVAIN
    摘要:Described herein is a peptide or peptidomimetic with a length of at least 6 residues comprising, consisting essentially of, or consisting of the sequence motif Xaa1-Trp-Xaa2-Xaa3-Xaa4-Xaa5 (SEQ ID NO:1), wherein: Xaa1 represents an aromatic residue (Phe, Tyr, Trp, His), Cys or Ser; Xaa2, Xaa3 and Xaa4 represent any residue; and Xaa5 represents Gly, lie or Val.

    专利号:EP-3070087-B1
    优先权日:2011-08-05
    标题 :Intermediates for the synthesis of cyclic p1 linkers as factor xia inhibitors

    专利号:EP-3070087-A1
    优先权日:2011-08-05
    标 题 :Intermediates for the synthesis of cyclic p1 linkers as factor xia inhibitors

    专利号:EP-2520573-A1
    优先权日:2011-05-06
    标 题:Compounds with matrix-metalloproteinase inhibitory activity
    发明人:HAUFE GUENTER; BEHRENDS MALTE; KOPKA KLAUS; WAGNER STEFAN; HUGENBERG VERENA; BREYHOLZ HANS-JOERG; HERMANN SVEN; SCHAEFERS MICHAEL; KOLB HARTMUTH
    权利人:UNIV MUENSTER WILHELMS; SIEMENS MEDICAL SOLUTIONS
    摘要:The present invention relates to the field of therapeutic and diagnostic agents and more specifically to compounds of formula (I) that are inhibitors of matrix-metalloproteinases (MMPs) and are useful in the treatment of diseases related thereto such as cardiovascular diseases, inflammatory diseases and malignant diseases. One embodiment of the invention is a compound of formula (I) labeled with a 18-fluorine atom having matrix metalloproteinase inhibitory activity suitable for diagnostic imaging. Also disclosed in the present invention is a pharmaceutical composition comprising the inhibitors of matrix-metalloproteinases (MMPs) of the invention or the corresponding labeled compounds useful as diagnostic imaging agents of the invention in a form suitable for mammalian administration. The invention furthermore discloses intermediates in the synthesis of the inhibitors of matrix-metalloproteinases (MMPs) of the invention and of the diagnostic imaging agents of the invention and kits for the preparation of the pharmaceutical composition of the invention.

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    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

    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):1793-1144.
    [参考文献]: Irena Berezowska, Et Al. Cyclic Opioid Peptide Agonists And Antagonists Obtained Via Ring-Closing Metathesis. Chem Biol Drug Des. 2009 Oct;74(4):329-34.
    [参考文献]: Pl Johnson, Et Al. Disruption Of Gabaergic Tone In The Dorsomedial Hypothalamus Attenuates Responses In A Subset Of Serotonergic Neurons In The Dorsal Raphe Nucleus Following Lactate-Induced Panic. J Psychopharmacol. 2008 Aug;22(6):642-52.
    [参考文献]: Stephan Urwyler, Et Al. Drug Design, In Vitro Pharmacology, And Structure-Activity Relationships Of 3-Acylamino-2-Aminopropionic Acid Derivatives, A Novel Class Of Partial Agonists At The Glycine Site On The N-Methyl-D-Aspartate (Nmda) Receptor Complex. J Med Chem. 2009 Aug 27;52(16):5093-107.
    [参考文献]: Tadashi Saigusa, Et Al. In Vivo Neurochemical Evidence That Newly Synthesised Gaba Activates Gaba(B), But Not Gaba(A), Receptors On Dopaminergic Nerve Endings In The Nucleus Accumbens Of Freely Moving Rats. Neuropharmacology. 2012 Feb;62(2):907-13.

    合成参考文献


    摘要:Hall, M.; Faber, K.; Tasnádi, G., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 1, 310.
    摘要:Hall, M.; Faber, K.; Tasnádi, G., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 1, 305.
    参考文献:10.1007/bf01388171
    摘要:Meffre P. Syntheses of optically active 2-amino-4-oxobutyric acid and N,O-protected derivatives. Amino Acids. 1999;16(3-4):251–72. doi: 10.1007/bf01388171.
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