Synthetic Route of 947249-27-6 , The common heterocyclic compound, 947249-27-6, name is 2-Bromo-3-(difluoromethoxy)pyridine, molecular formula is C6H4BrF2NO, 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.
Preparation 1032-Cvclopropyl-3-(difluoromethoxy)pyridineCyclopropylboronic acid (383 mg, 4.5 mmol) and potassium phosphate tribasic (1 .89g, 8.9 mmol) were added to a solution of 2-bromo-3-difluoromethoxypyridine (Preparation 102, 570 mg, 2.5 mmol). The mixture was heated to 80 C and degassed thoroughly by bubbling nitrogen through the mixture. After 30 minutes, the reaction was heated to 95 C and tricyclohexylphosphine (84 mg, 0.30 mmol) was added followed by palladium acetate (32 mg, 0.14 mmol). The reaction was stirred at 95 C for 18 hours then cooled to room temperature. The mixture was filtered through arbocel, washing with EtOAc and the filtrate concentrated in vacuo. The residue was then purified by flash column chromatography eluting with EtOAc:heptane 1 :5 to afford the title compound as a colourless oil (273 mg, 58%).1H NMR (400 MHz; DMSO-d6): delta 0.95 (m, 4H), 2.30 (m, 1 H), 7.05-7.42 (t, 1 H), 7.15 (m,1 H), 7.5 (m, 1 H), 8.25 (m, 1 H).LCMS Rt = 2.09 minutes MS m/z 186 [MH]+
The synthetic route of 947249-27-6 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; PFIZER LIMITED; BROWN, Alan Daniel; RAWSON, David James; STORER, Robert Ian; SWAIN, Nigel Alan; WO2012/7869; (2012); A2;,
Pyridine – Wikipedia,
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