Continuously updated synthesis method about 103977-79-3

The synthetic route of 103977-79-3 has been constantly updated, and we look forward to future research findings.

103977-79-3, name is 3-Bromo-2,4-difluoroaniline, belongs to bromides-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. Formula: C6H4BrF2N

To a mixture of 4,4,5,5,4′,4′,5′,5′-octamethyl-[2,2′]bi[[1,3,2]dioxaborolanyl] (1.831 g, 7.21 mmol), potassium acetate (1.415 g, 14.42 mmol) and [1,1′-bis(diphenylphosphino)ferrocene]dichloropalladium(II) complexed with dichloromethane (1:1) (0.785 g, 0.962 mmol) under nitrogen was added a solution of 3-bromo-2,4-difluoroaniline (1.0 g, 4.81 mmol) in 1,4-dioxane (20 mL). The mixture was stirred at 100 C. overnight. After cooling to room temperature, the mixture was diluted with DCM and filtered through Celite. The filtrated was concentrated in vacuo. The residue was purified by Biotage Isolera (740 mg, 60%). LCMS calculated for C12H17BF2NO2 (M+H)+ m/z=256.1; found 256.1.

The synthetic route of 103977-79-3 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Incyte Corporation; Vechorkin, Oleg; Pan, Jun; Liu, Kai; Sokolsky, Alexander; Wang, Anlai; Ye, Hai Fen; Ye, Qinda; Yao, Wenqing; (167 pag.)US2018/72720; (2018); A1;,
Bromide – Wikipedia,
bromide – Wiktionary