Ammonia → HCID 86680106, compound

Participants

Reaction Steps

A mixture of tert-butyl (R)-4-(4-(5-(tert-butoxycarbonylamino)-2-(2,6-difluorophenyl)thiazole-4-carboxamido)-1-(2,2,2-trifluoroethyl)-1H-pyrazol-5-yl)-2-methylpiperazine-1-carboxylate (82 mg, 0.12 mmol) in HCl/MeOH (10 mL) was stirred at ambient temperature for 20 hours. The reaction mixture was concentrated under reduced pressure to give a residue. The residue was diluted with MeOH (30 mL), neutralized with 28% ammonia solution, concentrated, and purified by preparative HPLC to afford 233 as a white solid (32 mg, 56%). 1H-NMR (500 MHz, CD3OD) δ (ppm): 7.69 (s, 1H), 7.51-7.45 (m, 1H), 7.17-7.12 (m, 2H), 4.84-4.78 (m, 2H), 3.22-3.17 (m, 1H), 3.05-2.86 (m, 6H), 1.08 (d, J=6 Hz, 3H); MS (ESI) m/z: 502 [M+H+].

Provenance & Evidence