These common heterocyclic compound, 104197-14-0, name is 4-Bromo-2,6-difluoroanisole, its 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. SDS of cas: 104197-14-0
To a solution of compound 5.2 (0.15 mL,1.22 mmol) in DME (7 mL) was added tetrakis triphenylphosphine palladium (78 mg,0.067 mmol). Stirring was continued at r.t. 5 min. 2-formyl phenyl boronic acid 5.1 (202 mg,1.35 mmol) and K2CO3 (745 mg,3.56 mmol) were added in turn. Stirring was continued at reflux 4h. The solvent was removed in vacuo. The crude was taken up with water and extracted with EtOAc (3 x 20 ml). The organic phase was washed with brine and dried over Na2S04. Flash chromatography purification (eluent PET/EtOAc) of the reaction crude afforded the title compound 5.3 (180 mg,0.72 mmol) as brownish oil.lH NMR (200 MHz,CDCI3) delta 4.20 (s,3H), 6.95 (d, / = 6.7 Hz,2H), 7.40 (d, / = 7.7 Hz,2H), 7.53 (d, / = 8.6 Hz,1H), 7.64-7.70 (m,1H), 8.03 (d, / = 7.8 Hz,1H), 10.02 (s,1H).
The synthetic route of 4-Bromo-2,6-difluoroanisole has been constantly updated, and we look forward to future research findings.
Reference:
Patent; TES PHARMA S.R.L.; PELLICCIARI, Roberto; (253 pag.)WO2018/69532; (2018); A1;,
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