📜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