📜Z-L-正缬氨酸置于palladium On Activated Charcoal 4-二甲氨基吡啶,氢气体系中,用 乙醇,叔丁醇 用作溶剂,化学反应 8.0H,反应生成L-正缬氨酸叔丁酯
参考文献:Synthesis Of Novel Potent Hepatitis C Virus Ns3 Protease Inhibitors: Discovery Of 4-Hydroxy-Cyclopent-2-Ene-1,2-Dicarboxylic Acid As A N-Acyl-L-Hydroxyproline Bioisostere
标题:Synthesis Of Novel Potent Hepatitis C Virus Ns3 Protease Inhibitors: Discovery Of 4-Hydroxy-Cyclopent-2-Ene-1,2-Dicarboxylic Acid As A N-Acyl-L-Hydroxyproline Bioisostere
摘要:Potent Tetrapeptidic Inhibitors Of The Hcv Ns3 Protease Have Been Developed Incorporating 4-Hydroxy-Cyclopent-2-Ene-1,2-Dicarboxylic Acid As A New N-Acyl-L-Hydroxyproline Mimic. The Hydroxycyclopentene Template Was Synthesized In Eight Steps From Commercially Available,(Syn)-Tetrahydrophthalic Anhydride. Three Different Amino Acids Were Explored In The Pi-Position And In The P2-Position The Hydroxyl Group Of The Cyclopentene Template Was Substituted With 7-Methoxy-2-Phenyl-Quinolin-4-Ol. The P3/p4-Positions Were Then Optimized From A Set Of Six Amino Acid Derivatives. All Inhibitors Were Evaluated In An In Vitro Assay Using The Full-Length Ns3 Protease. Several Potent Inhibitors Were Identified,The Most Promising Exhibiting A K-I Value Of 1.1 Nm. (C) 2006 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmc.2006.10.044