Triethylamine → 2-sec-Butylamino-6-methanesulfonyloxy-isonicotinic acid methyl ester

Participants

Reaction Steps

Add methanesulfonyl chloride (0.1 mL, 1.292 mmol) to a solution of 2-sec-butylamino-6-hydroxy-isonicotinic acid (242 mg, 1.016 mmol) and triethyl amine (0.25 mL, 1.793 mmol) in dichloromethane (15 mL) at 0° C. Stir at room temperature for 15 min, dilute with dichloromethane, wash with saturated aqueous sodium chloride, dry (magnesium sulfate), concentrate and purify (silica gel chromatography, eluting with 15:85 ethyl acetate:hexanes) to give the title compound as a white solid (240 mg, 75%).

Provenance & Evidence