📜5-溴-2-叔丁基嘧啶置于盐酸,Tris-(Dibenzylideneacetone)Dipalladium(0),R-(+)-1,1'-联萘-2,2'-双二苯膦,Sodium T-Butanolate体系中,用 四氢呋喃,5,5-Dimethyl-1,3-Cyclohexadiene,水 作为反应溶剂,化学反应 2.0H,反应生成 四苯基锡
参考文献:The Synthesis Of A Novel Inhibitor Of B-Raf Kinase
标题:The Synthesis Of A Novel Inhibitor Of B-Raf Kinase
摘要:A Scaleable Synthetic Route To [4,7']Bis-Isoquinolinyl-1-Yl-(2-Tert-Butyl-Pyrimidine-5-yl)Amine (1),An Inhibitor Of B-Raf Kinase Is Described. The Key Step In The Synthesis Is The Pd-Catalyzed Negishi Coupling Of 4-Bromo-1-Chloroisoquinoline With Trifluoromethanesulfonic Acid Isoquinoline-7-Yl Ester To Yield 1-Chloro-[4,7']Bis-Isoquinolinyl. This Intermediate Is Transformed To The Desired Drug Substance In One Additional Step,By Reaction With 2-Tert-Butyl-5-Aminopyrimidine In The Presence Of Nah. A Special Focus Was Put On The Finally Successful Removal Of Traces Of Zn And Pd In The Drug Substance,Which Came From The Negishi Coupling.
DOI:10.1021/op0501601