Picolinic acid → Ethyl chloroformate

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Reaction Steps

Picolinic acid compound 4 is reacted with an organic base, e.g., triethylamine, followed by an acid chloride, e.g., pivaloyl chloride or a chloroformate, e.g., C2H5OCOCl in a suitable solvent such as dichloromethane at a temperature of about −30° C. to 0° C. to give a mixed anhydride. To the mixture is added NH2R5 at a temperature of −30° C. to 0° C. either neat or as a solution in a suitable solvent to form amide compound 2.

Provenance & Evidence