- form White solid.
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.
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