对氯苯甲酸甲酯置于n-溴代丁二酰亚胺(Nbs),Lithium Aluminium Tetrahydride,硫酸体系中,用 乙醚 用作溶剂,化学反应 15.5H,反应生成(3-溴-4-氯苯基)甲醇
参考文献:Discovery Of Potent And Selective Sh2 Inhibitors Of The Tyrosine Kinase Zap-70
标题:Discovery Of Potent And Selective Sh2 Inhibitors Of The Tyrosine Kinase Zap-70
摘要:A Series Of 1,2,4-Oxadiazole Analogues Has Been Shown To Be Potent And Selective Sh2 Inhibitors Of The Tyrosine Kinase Zap-70,A Potential Therapeutic Target For Immune Suppression. These Compounds Typically Are 200-400-Fold More Potent Than The Native,Monophosphorylated Tetrapeptide Sequences. When Compared With The High-Affinity Xi-1-Itam Peptide (Ac-Nql-Pynelnlgrree-Pydvld-Nh2,Wherein Py Refers To Phosphotyrosine) Some Of The Best 1,2,4-Oxadiazole Analogues Are Approximately 1 Order Of Magnitude Less Active. This Series Of Compounds Displays An Unprecedented Level Of Selectivity Over The Closely Related Tyrosine Kinase Syk,As Well As Other Sh2-Containing Proteins Such As Src And Grb2. Gel Shift Studies Using A Protein Construct Consisting Only Of C-Terminal Zap-70 Sh2 Demonstrate That These Compounds Can Effectively Engage This Particular Sh2 Domain.
Doi:10.1021/jm990229T