6-(Thiophen-3-yl)-nicotinic acid synthesis

Yield:877674-90-3 68%

Reaction Conditions:

with formic acid;dihydrogen peroxide at 0; for 24 h;

Steps:

Procedure V: 6-Thiophen-3-yl-pyridine-3-carbaldehyde (0.475 g, 2.5 mmol) is suspended in formic acid (3.5 mL), and the solution is placed in an ice bath. Hydrogen peroxide is added (0.875 mL, 7.5 mmol), and the reaction vessel is placed in the refrigerator and is allowed to stand for 1 day. On addition of water, a white solid is precipitated, which is filtered, washed with cold water and dried in a vacuum oven to give the desired product (0.35 g, 68%). MS (ES-) 204.1.

References:

WO2006/23462,2006,A1 Location in patent:Page/Page column 54