CAS: 66147-29-3; (S)-4-(4-(((2,4-Diaminopteridin-6-yl)Methyl)(Methyl)Amino)Benzamido)-5-Methoxy-5-Oxopentanoic Acid

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6-bromomethyl-2,4-diaminopteridine hydrobromide (2S)-2-(4-methylaminobenzoylamino)pentanedioic acid 1-methyl ester 10-methylpteroyl)-L-glutamateα-methyl γ-tert-butyl N-(4-amino-4-deoxy-N10-methylpteroyl)-L-glutamate N-methyl-p-aminobenzoic acidtert-butyl ester6-(4-{4-[(2,4-diamino-pteridin-6-ylmethyl)-methyl-amino]-benzoylamino}-4-methoxycarbonyl-butyrylamino)-hexanoic acid tert-butyl ester 2-{4-[(2,4-diamino-pteridin-6-ylmethyl)-methyl-amino]-benzoylamino}-4-{2-[3,4,5-triacetoxy-6-(4,5,6-triacetoxy-2-acetoxymethyl-tetrahydro-pyran-3-yloxy)-tetrahydro-pyran-2-ylmethylsulfanyl]-ethylcarbamoyl}-butyric acid methyl ester 6-((S)-4-{4-[(2,4-Diamino-pteridin-6-ylmethyl)-methyl-amino]-benzoylamino}-4-methoxycarbonyl-butyrylamino)-hexanoic acid 2-{4-[(2,4-diamino-pteridin-6-ylmethyl)-methyl-amino]-benzoylamino}-4-{2-[3,4,5-triacetoxy-6-(4,5-diacetoxy-2-acetoxymethyl-6-fluoro-tetrahydro-pyran-3-yloxy)-tetrahydro-pyran-2-ylmethylsulfanyl]-ethylcarbamoyl}-butyric acid methyl ester

合成工艺路线路线简述

    📜6-溴乙基-喋啶-2,4-二胺置于三氟乙酸体系中,用 二氯甲烷,N,N-二甲基乙酰胺 作为反应溶剂,化学反应 7.0H,反应生成 甲氨蝶呤alpha-甲酯
    参考文献:Optimized Design And Synthesis Of Chemical Dimerizer Substrates For Detection Of Glycosynthase Activity Via Chemical Complementation
    标题:Optimized Design And Synthesis Of Chemical Dimerizer Substrates For Detection Of Glycosynthase Activity Via Chemical Complementation
    摘要:Glycosynthases Catalyze The Formation Of A Glycosidic Bond Between A Glycosyl Fluoride Donor Substrate And A Glycosyl Acceptor Substrate With High Yield,Thus Providing A Valuable Approach For The Synthesis Of Carbohydrates And Glycoconjugates. Chemical Complementation Can Be Used To Link Glycosynthase Activity To The Transcription Of A Reporter Gene In Vivo,Providing A Selection For The Directed Evolution Of Glycosynthase Enzymes With Improved Properties. In This Approach,Glycosynthase Activity Is Detected As Covalent Coupling Between A Small Molecule Disaccharide Acceptor Substrate And A Small Molecule Disaccharide Alpha-Fluoro Donor Substrate. Here We Report The Optimized Design And Synthesis Of These Small Molecule Substrates. These Optimized Substrates Are Shown To Give A Robust,Glycosynthase-Dependent Transcriptional Read-Out In The Chemical Complementation Assay. The Full Synthesis And Characterization Of These Substrates Are Reported For The First Time. These Optimized Chemical Dimerizer Substrates Should Allow The Potential Of Chemical Complementation For The Directed Evolution Of Glycosynthases With Diverse Substrate Specificities And Improved Properties To Be Fully Realized. (C) 2006 Elsevier Ltd. All Rights Reserved.
    DOI:10.1016/j.Bmc.2006.06.034

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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Henderson GB, Tsuji JM. Methotrexate efflux in L1210 cells. Kinetic and specificity properties of the efflux system sensitive to bromosulfophthalein and its possible identity with a system which mediates the efflux of 3',5'-cyclic AMP. J Biol Chem. 1987 Oct 5;262(28):13571-8.

    合成参考文献

    合成方法参考DOI号:10.1016/j.bmc.2006.06.034
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