These common heterocyclic compound, 887266-99-1, name is 3-Fluoro-4-iodobenzonitrile, 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. HPLC of Formula: C7H3FIN
A mixture of 3-fluoro-4-iodobenzonitrile (1.0 g, 4.06 mmol), trimethylsilyl acetylene (0.595 g,6.07 mmol), CuT (50 mg, 0.26 mmol), PdC12(PPh3)2 (50 mg, 0.07 1 mmol) and TEA (3 mL) in DMSO (7 mL) was stirred at RT for 16 h. After the reaction, the reaction mixture was quenched with water, extracted with EtOAc. The organic layer was washed with water, brine, dried over Na2SO4 and concentrated to afford 750 mg of crude 2-chloro-5-((trimethylsilyl)-ethynyl) benzoate. To this crude solution of 2-chloro-5-((trimethylsilyl)ethynyl)benzoate (500 mg, 1.87 mmol) in DCM (10 mL) was added TBAF (1.0 g, 3.83 mmol) and stirred further at RT for h. Then the reaction mixture was quenched with water, extracted with DCM, washed with water, brine, dried over Na2SO4 and concentrated to afford 450 mg of the title product. ?H NMR (300 MHz, CDC13): 7.61-7.56 (t, J= 7.2 Hz, 1H), 7.44-7.38 (d, J= 8.1 Hz,2H), 3.52(s, 1H).
The synthetic route of 3-Fluoro-4-iodobenzonitrile has been constantly updated, and we look forward to future research findings.