Trifluoroacetic acid → HCID 89810787, compound

Participants

Reaction Steps

To a solution of tert-butyl 4-(6-(6-chloro-5-(2,4-difluorophenylsulfonamido)pyridin-3-yl)pyrido[3,2-d]pyrimidin-4-ylamino)piperidine-1-carboxylate (1.28 g, 2.03 mmol) in DCM (20 mL) was added TFA (3.10 mL, 40.5 mmol) at 0° C. The reaction mixture was stirred for 4 h at room temperature and removed the solvent in vacuo. DCM was poured into the residue, and neutralized with aq. Na2HCO3. The resulting solid was filtered and washed with MeOH and EtOAc to give N-(2-chloro-5-(4-(piperidin-4-ylamino)pyrido[3,2-d]pyrimidin-6-yl)pyridine-3-yl)-2,4-difluorobenzenesulfonamide (954 mg, 89%) as a pale yellow solid. 1H-NMR (DMSO-d6, Varian 400 MHz) δ 1.84-2.00 (2H, m), 2.12-2.24 (2H, m), 3.04-3.18 (2H, m), 3.32-3.46 (2H, m), 4.38-4.52 (1H, m), 7.07 (1H, dt, J=2.0, 8.4 Hz), 7.22 (1H, dt, J=2.4, 10.0 Hz), 7.83-7.92 (1H, m), 8.04 (1H, d, J=8.0 Hz), 8.11 (1H, d, J=8.8 Hz), 8.19 (1H, d, J=8.8 Hz), 8.26 (1H, d, J=2.4 Hz), 8.43 (2H, brs), 8.52 (1H, s), 8.59 (1H, d, J=2.4 Hz). m/z=532.2 [M+1]+.

Provenance & Evidence