Continuously updated synthesis method about C8H5BrF2O2

773134-11-5, name is Methyl 4-bromo-2,6-difluorobenzoate, belongs to esters-buliding-blocks compound, is considered to be a conventional heterocyclic compound, which is widely used in drug synthesis. The chemical synthesis route is as follows. category: esters-buliding-blocks

773134-11-5, name is Methyl 4-bromo-2,6-difluorobenzoate, belongs to esters-buliding-blocks compound, is considered to be a conventional heterocyclic compound, which is widely used in drug synthesis. The chemical synthesis route is as follows. category: esters-buliding-blocks

Methyl 4-bromo-2,6-difluorobenzoate (Intermediate 5a, 502 mg, 2 mmol) was dissolved in A/,N-dimethylformamide (5 mL) and triethylamine (1 .59 mL, 10 mmol). The solution was purged with nitrogen for 5 min and copper(l)iodide (19 mg, 0.1 mmol) and bis(triphenylphosphine)palladium(ll)chloride (70.2 mg, 0.1 mmol) were added. The mixture was stirred for 5 min after which cyclohexylacetylene (1.29 mL, 10 mmol) was added and the reaction mixture was stirred at 80 C for 2 h. The reaction mixture was added to a stirred mixture of water/brine/ethyl acetate = 1/1/1 v/v% (45 mL). The organic layer was separated, washed with water, brine, dried over sodium sulfate, filtered and concentrated under reduced pressure. The crude residue was purified by column chromatography (heptane/ethyl acetate = 95/5 v/v%) to afford 360 mg of the title compound (yield: 64.7%).

The synthetic route of 773134-11-5 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; NETHERLANDS TRANSLATIONAL RESEARCH CENTER B.V.; DE MAN, Adrianus Petrus Antonius; UITDEHAAG, Joost Cornelis Marinus; STERRENBURG, Jan Gerard; DE WIT, Joeri Johannes Petrus; VAN CAUTER, Freek; SEEGERS, Nicole Wilhelmina Cornelia; VAN DOORNMALEN, Antonius Maria; BUIJSMAN, Rogier Christian; ZAMAN, Guido Jenny Rudolf; (89 pag.)WO2019/43103; (2019); A1;,
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