Lithium Hydroxide → 2-{[(1S)-1-(5-Fluoropyrimidin-2-yl)ethyl]amino}-6-[(5-methyl-1H-pyrazol-3-yl)amino]-5-nitropyrimidine-4-carboxylic acid

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To a solution of ethyl 2-{[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]amino}-6-[(5-methyl-1H-pyrazol-3-yl)amino]-5-nitropyrimidine-4-carboxylate (Intermediate 49, 2 mmol) in THF/MeOH (1:1 v/v, 10 ml) was added LiOH (0.42 g) in H2O (1 ml) and the resulting mixture was stirred at ambient temperature overnight. The volatiles were evaporated under reduced pressure and the solid left was diluted with H2O. The aqueous layer was acidified with 1N HCl (aq) solution and extracted with EtOAc (3×). The combined organic layers were dried and evaporation gave the title compound (406 mg), used in the next step without further purification. LCMS: 402 [M−1].

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