Methanol → 4-(4-Bromo-2-fluorophenylamino)-5-fluoro-6-methoxy-nicotinic acid methyl ester

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Reaction Steps

Sodium methoxide (2.20 g, 40.8 mmol) was slowly added to a stirred solution of 4-(4-bromo-2-fluorophenylamino)-6-chloro-5-fluoro-nicotinic acid methyl ester in 4:1 MeOH:THF (20 mL) at 0° C. The reaction mixture was warmed to room temperature, stirred for 17 hours and then warmed to 40° C. and stirred for 5 hours. After cooling to room temperature, the reaction mixture was quenched with water and extracted with ethyl acetate. The combined organic extracts were dried (MgSO4) and concentrated tinder reduced pressure. The desired product, contaminated with some starting material, was carried forward without purification.

Provenance & Evidence