Application of 133739-70-5,Some common heterocyclic compound, 133739-70-5, name is 1-Bromo-2,3,5-trifluorobenzene, molecular formula is C6H2BrF3, traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
Dissolve trifluoromethanesulfonic acid 1- [4- (2-azepan-1-yl-ethoxy)-benzoyl]-6- methoxynaphthalen-2-yl ester (2.60 g, 6.53 mmol) in 200 ml. acetonitrile and add to this bis (pinacoloato) diboron (1.5 g, 7.96 mmol), bis (tricyclohexylphosphine) palladium (0) (0.72 g, 1.50 mmol) and cesium fluoride (7.33 g, 67.0 mmol). Heat the reaction to 100 C until LC/MS indicates all starting material is consumed. Add to this mixture 1-bromo- 2,3, 5-trifluorobenzene (2.00 g, 13.06 mmol) and another 720 mg of palladium catalyst and heat at 80 C for 24 hours. Filter the reaction, concentrate and purify on a silica gel column eluting with a 0-10% methanol/methylene chloride gradient to give 1.85 g (53%) of the title compound.
The synthetic route of 133739-70-5 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; ELI LILLY AND COMPANY; WO2005/73204; (2005); A1;,
Bromide – Wikipedia,
bromide – Wiktionary