Triethylamine → 5-Propylpyrimidin-2-ylpiperidin-4-yl methanesulfonate

Participants

Reaction Steps

To a stirring solution of 1-(5-propylpyrimidin-2-yl)piperidin-4-ol (9.2 g, 41.6 mmol), Et3N (12.85 mL, 91 mmol, Aldrich) in CH2Cl2 (80 mL) at 0° C. was added a solution of Methanesulfonyl chloride (3.54 mL, 45.7 mmol, Acros) in CH2Cl2 (20 mL) dropwise. The reaction mixture was stirred at room temperature for 1 h and washed with 1N HCl in H2O, saturated NaHCO3 in H2O and brine. The organic layer was dried over Na2SO4 and concentrated in vacuo to yield 11.7 g of the desired product as an off-white solid. MS (ESI) 300 (M+H).

Provenance & Evidence