Methylamine → HCID 58504551, compound

Participants

Reaction Steps

The crude 4-chloro-2-(methylsulfonyl)-6-[(2S)-2-(trifluoromethyl)-1-pyrrolidinyl]pyrimidine (1.09 g, 3.31 mmol) was dissolved 1,4-dioxane (30 mL). Hunig's base (2.88 mL, 16.53 mmol) and methylamine (6.61 mL, 13.22 mmol) were added, and the solution was stirred at room temperature overnight. Additional methylamine (2 mL) was added. The reaction was concentrated, then diluted with 30 mL EtOAc and washed with 0.1 N HCl (30 mL). The aqueous was back extracted with EtOAc and the organics were combined and washed with saturated NaCl, dried over MgSO4, filtered and concentrated. Purfication on Biotage 25 g SNAP column with a gradient of 0 to 50% EtOAc in Hexane over 35 minutes afforded the title compound (760 mg) as a clear oil. LC-MS (ES) m/z=281 [M+H]+.

Provenance & Evidence