1H-Pyrazole-4-carboxamide,5-amino-1-ethyl-(9CI) synthesis

Yield:145864-65-9 78%

Reaction Conditions:

with sodium hydroxide;water;dihydrogen peroxide in methanol at 20; for 3 h;

Steps:

3

A mixture of 5 -amino- 1 -ethyl- lH-pyrazolo 4-carbonitrile 2b (630 mg, 4.65 mmol), IM aqueous solution of sodium hydroxide (1.1 equiv., 5.12 ml) and approximately 30% aqueous solution of hydrogen peroxide (5 equiv., 2.72 ml) were stirred in methanol (30 ml) at room temperature for 3 hours. The volume of reaction mixture was reduced in vacuo, precipitate filtered and dried to give 5 -amino- 1 -ethyl- lH-pyrazolo-4-carboxylic acid amide 3b (639 g, 78%).

References:

WO2009/97446,2009,A1 Location in patent:Page/Page column 66