Citric Acid → 4-Isopropylthiazole-2-carboxylic acid (6-carbamoyl-3-methoxy-2-methyl-phenyl)-amide

Participants

Reaction Steps

To a stirred mixture of 2-amino-4-methoxy-3-methyl-benzamide (2.0 g, 11 mmol), 4-isopropyl-thiazole-2-carboxylic acid (2.4 g, 14 mmol) and Hobt-hydrate (2.2 g, 14 mmol) in dry DMF (80 ml) was added EDAC (2.88 g, 15 mmol) and TEA (2.1 ml, 15 mmol) and the mixture was stirred overnight. A 5% aqueous solution of citric acid was added and the mixture was extracted three times with ethyl acetate. The organic phase was washed with saturated sodium hydrogen carbonate solution (two times) and brine, dried with sodium sulfate and evaporated under reduced pressure which gave the title compound (3.1 g).

Provenance & Evidence