Synthesis
General procedure for the synthesis of 2-fluorobenzylamine from 2-fluorobenzonitrile: the standard method for the reduction of nitrile by KBH4 and CuCl2 was used. The procedure was as follows: 2-fluorobenzonitrile (0.15 g, 1 mmol), KBH4 (0.17 g, 3 mmol), CuCl2 (0.03 g, 0.25 mmol), and 80% isopropanol solution (1.6 mL of isopropanol and 0.4 mL of water) were added to a 10 mL round-bottom flask. The reaction was carried out at 60 °C and the progress of the reaction was monitored by TLC (unfolding agent ratio of DCM:MeOH 10:1) to confirm that the reaction was completed within 8 hours. Upon completion of the reaction, the mixture was cooled to 25 °C and the solvent was subsequently removed under reduced pressure. Ethyl acetate (5 mL) was added to the residue and washed sequentially with water (1 mL) and saturated saline (1 mL). The organic layer was dried over anhydrous Na2SO4, filtered and concentrated under reduced pressure to give the crude product 2-fluorobenzylamine.
References
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