Potassium Hydroxide → 1-(4-((1-(tert-Butoxycarbonyl)piperidin-3-yl)methylamino)-6-(5-cyanopyrazin-2-ylamino)pyridin-3-yl)-1H-pyrrole-3-carboxylic acid

Participants

Reaction Conditions

Reaction Steps

tert-Butyl 3-((2-(5-cyanopyrazin-2-ylamino)-5-(3-(ethoxycarbonyl)-1H-pyrrol-1-yl)pyridin-4-ylamino)methyl)piperidine-1-carboxylate (42 mg, 0.077 mmol) was dissolved in ethanol (1 mL). KOH (43 mg, 0.770 mmol) was added and the solution was stirred at 50° C. for 72 h. The reaction mixture was evaporated to dryness and the residue was partitioned between water and dichloromethane. The two phases were separated and the organic phase was extracted with water. The combined aqueous phases were neutralised to pH 7 by the addition of 1M HCl and then evaporated to dryness. The product (7 mg, 17%) was used directly in the next step without further purification.

Provenance & Evidence