Hydrochloric Acid → HCID 59232146, compound

Participants

Reaction Steps

A solution of tert-butyl 2-({4-amino-5-[3-fluoro-4-({[2-fluoro-5-(trifluoromethyl)phenyl]carbamoyl}amino)phenyl]pyrrolo[2,1-f][1,2,4]triazin-7-yl}carbonyl)morpholine-4-carboxylate (50 mg, 0.076 mmol) in 1,4-dioxane (1 mL) was treated with 4N HCl (200 μL) in 1,4-dioxane and stirred at rt for 4 h. The reaction was concentrated then diluted with EtOAc and saturated NaHCO3 solution. The organic layer was dried (MgSO4) and concentrated. The crude residue was triturated with EtOAc and filtered. A yellow solid was isolated (24 mg, 57%). 1H-NMR (CD3OD) δ 8.65 (d, J=8.2 Hz, 1 H), 8.32 (t, J=8.5 Hz, 1 H), 8.09 (s, 1 H), 7.48 (s, 1 H), 7.34-7.29 (m, 4 H), 5.26 (dd, J1=9.6 Hz, J2=2.6 Hz, 1 H), 4.65-4.60 (m, 1H), 4.00 (dt, J1=11.6 Hz, J2=2.5 Hz, 1 H), 3.82-3.75 (m, 1 H), 2.89-2.86 (m, 2 H), 2.75 (dd, J1=12.8 Hz, J2=9.6 Hz, 1 H); MS [M+H]+=562.1; LCMS RT=2.66 min.

Provenance & Evidence