Dichloromethane → (S)-4-(4,6-Dichloropyrimidin-2-yl)-3-methylmorpholine

Participants

Reaction Steps

To a solution of trichloropyrimidine (5.04 g, 27.3 mol) in DCM (50 mL) cooled to 0° C. was added DIPEA (4.79 mL, 27.3 mol), followed by 3-(S)-methylmorpholine (3.11 g, 30.5 mol) dropwise. The reaction mixture was allowed to warm to RT and stirred for 3 h wherupon it was diluted with DCM, washed with water and brine, dried over magnesium sulfate, filtered and the solvent removed in vacuo. The residue was purified by flash chromatography (5-10% EtOAc in petroleum ether (40-60)) to yield the two isomers.

Provenance & Evidence