Methylamine → HCID 86659173, compound

Participants

Reaction Conditions

Reaction Steps

To cis-1-[6-chloro-2-(methylsulfonyl)-4-pyrimidinyl]-N-cyclohexyl-6-(trifluoromethyl)-3-piperidinecarboxamide (390 mg, 0.832 mmol) in 1,4-dioxane (8 mL) was added Hunig's base (0.29 mL, 1.66 mmol) followed by 2M methylamine in THF (1 mL, 2 mmol), and the reaction mixture was stirred overnight at 60° C. into a sealed tube. The mixture was poured onto water and EtOAc. The organic layer was separated, washed with brine, dried (MgSO4), filtered and concentrated. Flash chromatography on SiO2 (gradient: 100% Hexanes to 50% EtOAc in Hexanes) afforded the title compound (204 mg) as a white foam. LC-MS (ES) m/z=420, 422 [M+H]+.

Provenance & Evidence