Oxalyl chloride → 6-Chloro-4-pyrimidinecarboxylic acid

Participants

Reaction Conditions

Reaction Steps

To a solution of 6-hydroxypyrimidine-4-carboxylic acid (6.0 g, 42.8 mmol) in EtOAc (90 mL) was added (COCl)2 (12 mL) dropwise, followed by a few drops of DMF. The mixture was stirred at 75° C. for 3 h, and then at 25° C. for 16 h. The solvent was evaporated to give the crude 6-chloropyrimidine-4-carboxylic acid (6.3 g, yield: 92.9%). 1H NMR (400 MHz, DMSO-d6) δ 8.31 (s, 1H), 6.88 (s, 1H).

Provenance & Evidence