Ammonium formate → 4-Amino-3-{[1-(tetrahydro-2H-pyran-4-yl)-4-piperidinyl]amino}-benzonitrile

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Reaction Steps

4-Nitro-3-{[1-(tetrahydro-2H-pyran-4-yl)-4-piperidinyl]amino}benzonitrile (D58, 592 mg, 0.0018 mol, 1 eq), 10% palladium on carbon (200 mg, 0.00018 mol, 0.1 eq), ammonium formate (375 mg, 0.0057 mol, 3.2 eq), and methanol (15 ml) (degassed with nitrogen) were combined and stirred for 1 hour. The catalyst was then filtered off, and the reaction evaporated, water and dichloromethane added and shaken. Separation and drying of the dichloromethane layer with sodium sulfate followed by evaporation yielded a crude product which was purified exactly as in Example 1 where A=H2O and B=acetonitrile to afford the title compound. MS (ESI): 301 [M+H]+

Provenance & Evidence