Acetic Anhydride → 2-Chloro-6-formylaminomethylnicotinic acid methyl ester

Participants

Reaction Steps

To a solution of 6-aminomethyl-2-chloro-nicotinic acid methyl ester (740 mg, 3.7 mmol) in formic acid (18.5 mL) was added acetic anhydride (3.7 mL). The reaction mixture was stirred at room temperature for 1.5 hours. The reaction mixture was concentrated in vacuo and azeotroped three times with toluene to afford the title compound as a yellow oil (757 mg, 90%) which was used without purification in the next step. LCMS (method B): RT=2.20 min, [M+H]+=229.

Provenance & Evidence