CAS: 382638-00-8; (S)-3-Tert-Butoxycarbonylamino-4-Methanesulfonyloxybutanoic Acid Methyl Ester

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    上下游产品

    (S)-3-(Boc-氨基)-4-羟基丁酸甲酯 Methyl (3S)-3-(Tert-Butoxycarbonylamino)-4-Hydroxybutanoate 136703-59-8
    (S)-N-Boc-3-氨基-4-羟基丁酸 (S)-3-((Tert-Butoxycarbonyl)Amino)-4-Hydroxybutanoic Acid 83345-44-2
    Boc-L-天冬氨酸 4-甲酯 (S)-2-T-Butoxycarbonylaminosuccinic Acid 4-Methyl Ester 59768-74-0
    Benzyl (3S)-3-[(Tert-Butoxycarbonyl)Amino]-4-Hydroxybutanoate 79069-16-2

    合成工艺路线路线简述

      📜Benzyl (3S)-3-[(Tert-Butoxycarbonyl)Amino]-4-Hydroxybutanoate置于palladium 10% On Activated Carbon,氢气,三乙胺体系中,用 四氢呋喃,甲醇,二氯甲烷 作为反应溶剂,化学反应 2.0H,反应生成 西他列汀杂质
      参考文献:Design,Synthesis And Sar Of Novel Ethylenediamine And Phenylenediamine Derivatives As Factor Xa Inhibitors
      标题:Design,Synthesis And Sar Of Novel Ethylenediamine And Phenylenediamine Derivatives As Factor Xa Inhibitors
      摘要:We Previously Reported On A Series Of Cyclohexanediamine Derivatives As Highly Potent Factor Xa Inhibitors. Herein,We Describe The Modification Of The Spacer Moiety To Discover An Alternative Scaffold. Ethylenediamine Derivatives Possessing A Substituent At The C1 Position In S Configuration And Phenylenediamine Derivatives Possessing A Substituent At The C5 Position Demonstrated Moderate To Strong Anti-Fxa Activity. Further Sar Studies Led To The Identification Of Compound 30H Which Showed Both Good In Vitro Activity (Fxa Ic50 = 2.2 Nm,Ptct2 = 3.9 Mu M) And In Vivo Antithrombotic Efficacy. (C) 2011 Elsevier Ltd. All Rights Reserved.
      DOI:10.1016/j.Bmcl.2011.01.132

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