Morpholine → HCID 11453778, compound

Participants

Reaction Steps

A mixture of [5-(4-fluoro-benzenesulfonyl)-2-methyl-pyrimidin-4-yl]-(2,4,6-trimethylphenyl)-amine (100 mg, 0.26 mmol) and morpholine (5 mL) was heated at reflux under N2 for 2 h, and then cooled to room temperature. The mixture was concentrated in vacuo, and the residue was dissolved in EtOAc, washed with water and brine, dried over Na2SO4, filtered and concentrated in vacuo. The residue was purified by chromatography on silica gel (EtOAc) to provide the target compound (108 mg, 92%) as a white solid: mp 221–223° C.; 1H NMR (500 MHz, CDCl3) δ 8.71 (s, 1H), 8.24 (br s, 1H), 7.80 (d, J=9.0 Hz, 2H), 6.91 (s, 2H), 6.88 (d, J=9.0 Hz, 2H), 3.83 (t, J=5.0 Hz, 4H), 3.29 (t, J=5.0 Hz, 4H), 2.37 (s, 3H), 2.30 (s, 3H), 2.03 (s, 6H); APCI MS m/z 453 [(M+H)+, calcd for C24H29N4O3S, 453.2].

Provenance & Evidence