Trifluoroacetic acid → N-(3-methoxy-4-(4-methyl-1H-imidazol-1-yl)phenyl)-8-phenyl-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-2-amine

Participants

Reaction Steps

Trifluoroacetic acid (0.238 mL, 3.09 mmol) was added dropwise to a stirred solution of tert-butyl 2-(3-methoxy-4-(4-methyl-1H-imidazol-1-yl)phenylamino)-4-(2-(tetrahydrofuran-2-yl)ethyl)-7,8-dihydropyrido[4,3-d]pyrimidine-6(5H)-carboxylate (0.330 g, 0.62 mmol) in DCM (3 mL) at rt. The reaction mixture was stirred under reflux for 1 hr. Five equivalents of trifluoroacetic acid were added and the reaction mixture was stirred at reflux for 1 hour. The reaction mixture was allowed to cool to room temperature. The organic mixture was washed with potassium carbonate (aq) and the organic layer was separated, dried (MgSO4) and concentrated giving 0.247 g (92%) of N-(3-methoxy-4-(4-methyl-1H-imidazol-1-yl)phenyl)-8-phenyl-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-2-amine.

Provenance & Evidence