3-溴-4-氟苯甲酸置于tris(Dibenzylideneacetone)Dipalladium(0) Chloroform Complex,硫酸,Caesium Carbonate,4,5-双二苯基膦-9,9-二甲基氧杂蒽,三氟乙酸体系中,用 二氯甲烷 用作溶剂,化学反应 2.0H,反应生成3-氨基-4-氟苯羧酸甲酯
参考文献:Discovery Of Dabrafenib: A Selective Inhibitor Of Raf Kinases With Antitumor Activity Against B-Raf-Driven Tumors
标题:Discovery Of Dabrafenib: A Selective Inhibitor Of Raf Kinases With Antitumor Activity Against B-Raf-Driven Tumors
摘要:Hyperactive Signaling Of The Map Kinase Pathway Resulting From The Constitutively Active B-Raf(V600E) Mutated Enzyme Has Been Observed In A Number Of Human Tumors,Including Melanomas. Herein We Report The Discovery And Biological Evaluation Of Gsk2118436,A Selective Inhibitor Of Raf Kinases With Potent In Vitro Activity In Oncogenic B-Raf-Driven Melanoma And Colorectal Carcinoma Cells And Robust In Vivo Antitumor And Pharmacodynamic Activity In Mouse Models Of B-Raf(V600E) Human Melanoma. Gsk2118436 Was Identified As A Development Candidate,And Early Clinical Results Have Shown Significant Activity In Patients With B-Raf Mutant Melanoma.
Doi:10.1021/ml4000063