Trifluoroacetic acid → (R)-5-cyclopropyl-N-(3-fluoro-4-(morpholin-2-yl)phenyl)pyrimidin-2-amine

Participants

Reaction Conditions

Reaction Steps

To a stirred solution of (R)-tert-butyl 2-(4-(5-cyclopropylpyrimidin-2-ylamino)-2-fluorophenyl)morpholine-4-carboxylate (180 mg) in acetonitrile (2 ml) and water (6 ml) was added trifluoroacetic acid (335 μl). The reaction mixture was then capped and the mixture was shaken at 80° C. for 16 h. The reaction mixture was then cooled to room temperature and poured into EtOAc and washed with 4 M aq. NaOH. The organic layer was dried over Na2SO4 and concentrated in vacuo. The crude material was purified by flash column chromatography (silica gel; gradient: CH2Cl2/MeOH/aq. NH3) to afford (R)-5-cyclopropyl-N-(3-fluoro-4-(morpholin-2-yl)phenyl)pyrimidin-2-amine (57 mg, xx %) as an off-white solid. MS (ISP): 315.2 ([M+H]+).

Provenance & Evidence