Methyl 2-(6-cyano-5-fluoropyridin-3-yl)-6-fluorobenzoate → Methyl 2-[6-(aminomethyl)-5-fluoropyridin-3-yl]-6-fluorobenzoate

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Reaction Steps

To a stirred solution of the above ester (0.75 g, 2.7 mmol) in NH3/MeOH (5 mL, 2.0 M) was added Raney 2800 nickel (slurry in water). The mixture was stirred under a H2 atmosphere (balloon) at room temperature for 6 hours. The mixture was then filtered through glass filter paper, washing with additional MeOH. The resultant solution was concentrated under vacuum and azeotroped three times with toluene to provide crude title compound (0.65 g, 2.34 mmol).

Provenance & Evidence