Basic information Description Safety Related Supplier
ChemicalBook >  Product Catalog >  Pharmaceutical intermediates >  Bulk Drug Intermediates >  Dabrafenib Mesylate(GSK-2118436B)

Dabrafenib Mesylate(GSK-2118436B)

Basic information Description Safety Related Supplier
Dabrafenib Mesylate(GSK-2118436B) Basic information
Dabrafenib Mesylate(GSK-2118436B) Chemical Properties
  • form White solid.
Dabrafenib Mesylate(GSK-2118436B) Usage And Synthesis
  • Description

    Dabrafenib Mesylate is a salt form of Dabrafenib. Dabrafenib is an inhibitor of certain mutated forms of BRAF kinase, several of which may be associated with stimulating tumour growth (e.g. the BRAF V600E mutation), and Dabrafenib is also an inhibitor of BRAF V600-mutation positive cancer cell growth, both in vitro and in vivo.

  • DescriptionDabrafenib mesylate, sold by GlaxoSmithKline under the trade name Tafinlar, was approved by the U.S. FDA in May 2013 for the treatment of metastatic BRAF-mutant melanoma. Dabrafenib reversibly inhibits the BRAF(V600E) mutant kinase as a selective ATP-competitive inhibitor which results in tumor regression.
  • DefinitionChEBI: A methanesulfonate (mesylate) salt prepared from equimolar amounts of dabrafenib and methanesulfonic acid. Used for treatment of metastatic melanoma.
  • Chemical SynthesisCommercially available fluoroaniline 40 was first converted to sulfonamide 42 in 91% yield by treatment with 2,5-difluorobenzenesulfonyl chloride (41) in the presence of pyridine. Next, deprotonation of 2-chloro-4-methylpyrimidine (43) with lithium bis(trimethylsilyl)amide (LHMDS) followed by addition to ester 42 afforded chloropyrimidine 44 in 72% yield. Bromination followed by thiazole formation through the use of 2,2-dimethylpropanethioamide gave the penultimate target 45 in 80% over two steps. Chloropyrimidine 45 was subjected to SNAr conditions with ammonium hydroxide to furnish the aminopyrimidine in 88% yield, and this was followed by exposure to methanesulfonic acid to afford dabrafenib mesylate (VI) in 85% yield.

Dabrafenib Mesylate(GSK-2118436B)(1195768-06-9)Related Product Information
Dabrafenib Mesylate(GSK-2118436B)SupplierMore
  • Company Name:Xuzhou zuncheng chemical technology co. LTD Gold
  • Tel:13813462880
  • Email:451247499@qq.com
  •  
  • Company Name:Shanghai Drjart Biological Co., Ltd. Gold
  • Tel:18616739945
  • Email:tianxiao549423850@163.com
  •  
  • Company Name:Jurong Coupling Biotechnology Co., Ltd. Gold
  • Tel:13656108824
  • Email:278191416@qq.com
  •  
  • Company Name:Twochem Co.Ltd Gold
  • Tel:15800915896 021-58111628-
  • Email:sales@twochem.com
  •  
  • Company Name:Ningbo Risheng Pharmaceutical Technology Co., Ltd. Gold
  • Tel:19906600019
  • Email:2928184953@qq.com
  •  
Related articles