3-Amino-5-bromobenzofuran-2-carboxamide synthesis

Yield:309922-87-0 91%

Reaction Conditions:

with potassium hydroxide in ethanol; for 1.5 h;Reflux;

Steps:

2 Exam pie 2. Preparation of 3-am i no-5-bromobenzofuran-2-carboxamide

1.00 mmol of 2-(4-bromo-2-cyanophenoxy)acetamide was added with 5.0 mL of potassium hydroxide in ethanolic solution (0.70 M) and the so obtained mixture was heated under reflux for 1.5 hour. After cooling, the solvent was evaporated under reduced pressure and the obtained residue was added with water. The solid that separates was collected by filtration, dried under vacuum and purified by crystallizationfrom acetone. 232.1 mg of the desired product of the title were so obtained (yield 91%). This product was characterized by chemical-physical and spectroscopic data.M.p. (°C): 220-222. 1H-NMR (o, DMSO, d6): 6.030 (5, 2H, NH, exc.), 7.327 (as, 2H, NH, exc.), 7.425 (d, 1H, Ar, J=8.81), 7.564 (dd, 1H, Ar, J=1.33, J=8.81), 8.074 (d,1H, Ar, J=2.24).

References:

WO2018/189683,2018,A1 Location in patent:Page/Page column 17