Morpholine → HCID 10437846, compound

Participants

Reaction Steps

2-(Methylsulfonyl)-4-(3,4-difluorobenzyloxy)-5-[4-chlorophenyl]-6-[2,4-dichlorophenyl]pyrimidine (Reference Example 6, 48 mg, 0.085 mmol) was reacted in excess neat morpholine at 80° for 3 h by the general procedure described in Example 31, Step A. Workup (solvent removal under reduced pressure, then toluene azeotrope) and flash column chromatography on silica gel (eluted with 88/12 hexanes/ethyl acetate) afforded the title product. HPLC/MS: m/e=564 (M++1); Rt=5.00 min 1H-NMR 500 MHz (CDCl3): δ 3.80 (m, 4H), 3.86 (m, 4H), 5.38 (s, 2H), 7.02 (d, J=8 Hz, 2H), 7.08-7.20 (m, 7H), 7.31(d, J=1 Hz, 1H).

Provenance & Evidence