Formic Acid → 4-[({7-[(2,6-Difluorobenzyl)oxy]-2,5-dimethylpyrazolo[1,5-a]pyridin-3-yl}carbonyl)amino]bicyclo[2.2.2]octane-1-carboxylic Acid

Participants

Reaction Conditions

Reaction Steps

56 mg (0.113 mmol) of methyl 4-[({7-[(2,6-difluorobenzyl)oxy]-2,5-dimethylpyrazolo[1,5-a]pyridin-3-yl}carbonyl)amino]bicyclo[2.2.2]octane-1-carboxylate from Example 152 were dissolved in 1.1 ml of THF/methanol (5/1), and 8.1 mg (0.339 mmol) of lithium hydroxide were added. The mixture was stirred at 40° C. for 10 h. After cooling, the mixture was acidified with 20 μl of formic acid and purified by means of preparative HPLC (RP18 column, eluent:acetonitrile/water gradient with addition of 0.05% formic acid). 41 mg of the target compound were obtained (75% of theory).

Provenance & Evidence