Ammonium formate → HCID 131734221, compound

Participants

Reaction Steps

Benzyl-4-[5-{2-[(tert-butoxycarbonyl)amino]pyridin-4-yl}-4-(3-{[(2,5-difluorophenyl)sulfonyl]-(methoxymethyl)amino}-2-fluorophenyl)-1,3-thiazol-2-yl]piperidine-1-carboxylate (prepared as described in Example 10, 110 mg, 0.13 mmol) was dissolved in absolute ethanol (10 mL) under nitrogen atmosphere. Ammonium formate (440 mg, 7 mmol) and palladium on charcoal 5% (150 mg portionwise) were then added. The mixture was refluxed for 2 days, then filtered on a celite pad and evaporated to dryness. The residue was taken up with DCM and washed with water. The organic layer was dried over Na2SO4 and evaporated, affording 75 mg (84%) of tert-butyl-{4-[4-(3-{[(2,5-difluorophenyl)sulfonyl]-(methoxymethyl)amino}-2-fluorophenyl)-2-(piperidin-4-yl)-1,3-thiazol-5-yl]pyridin-2-yl}carbamate.

Provenance & Evidence