Trifluoroacetic acid → HCID 178480425, compound

Participants

Reaction Conditions

Reaction Steps

0.5 mL of trifluoroacetic acid is added to a solution of 60 mg of N-[3-[5-fluoro-6-(4-methylperhydro-1,4-diazepin-1-yl)-1H-benzimidazol-2-yl]-1-(tetrahydro-pyran-2-yl)-1H-pyrazol-4-yl]piperidine-1-carboxamide in solution in 1 mL of dichloromethane. The reaction medium is stirred at 22° C. for 16 hours. The reaction medium is concentrated under vacuum in a rotary evaporator. After evaporation, the reaction crude is purified by flash chromatography. The elution is carried out with pure dichloromethane and then with a mixture of dichloromethane containing 5% of ammoniacal methanol. 29 mg of N-{3-[5-fluoro-6-(4-methylperhydro-1,4-diazepin-1-yl)-1H-benzimidazol-2-yl]-1H-pyrazol-4-yl}piperidine-1-carboxamide are obtained in the form of a yellow solid. 1H NMR (400 MHz, DMSO-d6, δ in ppm): 1.42 to 2.27 (m, 8H); 2.90 (s, 3H); from 3.18 to 3.65 (m, 12H); 7.20 (d, J=7.0 Hz, 1H); 7.56 (d, J=12.0 Hz, 1H); 8.00 (s, 1H). ES mass spectrum: m/z=439 (M−H)—base peak.

Provenance & Evidence