Trifluoroacetic acid → HCID 86670641, compound

Participants

Reaction Steps

Trifluoroacetic acid (1 mL) was added to a solution of 5-fluoro-1-{(3R)-3-(methylsulfonyl)-3-[(tetrahydro-2H-pyran-2-yloxy)amino]butyl}-4-[4-(oxetan-3-yloxy)phenyl]pyridin-2(1H)-one (164 mg, 0.304 mmol) in DCM (10 mL). The reaction was allowed to stir at rt overnight and then concentrated under vacuum. The residue was re-dissolved in dichloromethane and n-heptane and concentrated again to afford the title compound as a solid. (113 mg, 82%). MS (LCMS) m/z 455.1 (M+1). 1H NMR (400 MHz, METHANOL-d4) δ ppm 1.69 (s, 3H) 2.35 (ddd, J=13.66, 10.63, 5.17 Hz, 1H) 2.53-2.67 (m, 1H) 3.09 (s, 3H) 3.91 (ddd, J=12.98, 10.63, 5.27 Hz, 1H) 4.16-4.30 (m, 1H) 4.69 (dd, J=7.51, 4.78 Hz, 2H) 5.02 (t, J=6.73 Hz, 2H) 5.33 (t, J=5.46 Hz, 1H) 6.58 (d, J=7.42 Hz, 1H) 6.85-6.91 (m, 2H) 7.55 (dd, J=8.68, 1.85 Hz, 2H) 7.80 (d, J=6.24 Hz, 1H).

Provenance & Evidence