Electric Literature of 53312-81-5,Some common heterocyclic compound, 53312-81-5, name is 5-Amino-2-fluorobenzonitrile, molecular formula is C7H5FN2, 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.
Example 2: 2-Fluoro-5-[5-(3-morpholin-4-ylphenoxy)-pyrimidin-2-ylamino]- benzo-nitrile A suspension of 4-[3-(2-chloro-pyrimidin-5-yloxy)phenyl]morpholine (150 mg, 0.515 mmol), 5-amino-2-fluorobenzonitrile (70.2mg, 0.515mmol), in’5′(dibenzylideneacetone)-palladium(0) (23.6mg, 0.025mmol), 4,5- bi5′(diphenylphosphino)-9,9- dimethylxanthene (30mg, 0.0515mmol) and cesium carbonate (336mg, 1.03mmol) in degassed 1,4-dioxane (4mL) was heated at 80C for 2 days. The suspension was diluted with ethyl acetate and washed with water and brine. The organic phase was dried (MgS04) and the solvent removed under reduced pressure. The crude product was purified by column chromatography on silica (ethyl acetate:hexane 1: 1) to afford 2-fluoro-5-[5-(3-morpholin-4-ylphenoxy)pyrimidin-2- ylamino]benzonitrile as a light yellow solid (70mg, 35%).Mass: (ES+) 392 (M+H)+ HPLC: 97%NMR: 5H (d6-DMSO) 3.08 (4H, m), 3.69 (4H, m), 6.39 (1H, dd), 6.61 (1H, br s), 6.70 (1H, dd), 7.18 (1H, t), 7.47 (1H, t), 7.95 (1H, m), 8.30 (1H, m), 8.44 (2H, s) and 10.10 (1H, s).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 5-Amino-2-fluorobenzonitrile, its application will become more common.