HCID 178457927, compound → HCID 178457932, compound

Participants

Reaction Steps

A solution of 550 mg of 3-[3-(5-fluoro-6-morpholin-4-yl-1H-benzimidazol-2-yl)-1-(tetrahydropyran-2-yl)-1H-pyrazol-4-yl]-1,1-diisopropylurea in 8.5 mL of concentrated hydrochloric acid is stirred at ambient temperature for 12 hours and the medium is concentrated under vacuum in a rotary evaporator. The reaction crude is purified by preparative LC/MS, elution being carried out with a mixture of water and acetonitrile containing respectively 0.07% of trifluoroacetic acid. 183 mg of 3-[3-(5-fluoro-6-morpholin-4-yl-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-diisopropylurea in the form of a trifluoroacetate salt are isolated. 1H NMR (400 MHz, DMSO-d6, δ in ppm): 1.35 (d, J=7.0 Hz, 12H); 3.00 (m, 4H); 3.78 (m, 4H); 4.07 (m, 2H); 7.08 (broad d, J=7.5 Hz, 1H); 7.32 (broad d, J=12.0 Hz, 1H); 8.03 (s, 1H); 9.57 (s, 1H); 12.95 (broad m, 2H).

Provenance & Evidence