Methanol → 2-chloro-5-fluoro-N-methylpyrimidin-4-amine

Participants

Reaction Steps

To a 250 mL round bottom flask equipped with a stir bar was added 5-fluoro-2,4-dichloro-pyrimidine (9 g), methanol (40 mL) and 8M methylamine in ethanol (15 mL). The reaction heated up (mild exo-therm) and was allowed to stir at room temperature for 30 minutes. A check by TLC (1:1 EtOAc:heptane) and LCMS showed complete reaction. The reaction was concentrated down to give 9.77 g crude material which was purified on a silica column running a gradient of 1% to 10% MeOH in DCM over 35 minutes to give 2-chloro-5-fluoro-N-methylpyrimidin-4-amine (6.77 g).

Provenance & Evidence