Some common heterocyclic compound, 859855-53-1, name is 3-Amino-4-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. Application In Synthesis of 3-Amino-4-fluorobenzonitrile
Intermediate 28: (4-Fluoro-3-(pyrrolidin-l-yl)phenyl)methanamineStep 1: 4-Fluoro-3-(pyrrolidin-l-yl)benzonitrile3-Amino-4-fluorobenzonitrile (0.5 g, 3.67 mmol), 1 ,4-dibromobutane (0.439 ml, 3.67 mmol), sodium carbonate (0.779 g, 7.35 mmol) and toluene (3 ml) were added into a microwave vial. The resulting mixture was heated by microwave irradiation at 140 C for 2 hours. 1 ,4-dibromobutane (0.5 ml, 4.18 mmol) was added and the reaction mixture was irradiated at 140 C and at 160 C until the reaction had clearly stopped. The reaction mixture was diluted with dichloromethane and washed twice with water. The organic phase was dried over Na2S04, filtered and evaporated. The crude product was purified by column chromatography. 0.221 g of the title compound was obtained. NMR (400 MHz, CDC13) delta ppm 1.96 – 2.00 (m, 4 H) 3.39 – 3.48 (m, 4 H) 6.84 (dd, 1 H) 6.89 – 6.94 (m, 1 H) 6.96 – 7.04 (m, 1 H)
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 859855-53-1, its application will become more common.
Reference:
Patent; ORION CORPORATION; ARVELA, Riina; HOLM, Patrik; PIETIKAeINEN, Pekka; ROSLUND, Mattias; VAeISAeNEN, Emilia; WOHLFAHRT, Gerd; WO2012/152983; (2012); A1;,
Nitrile – Wikipedia,
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