Hydrochloric Acid → [1,2,4]Triazolo[1,5-a]pyridin-2-amine, 8-(3,4-difluorophenyl)-6-fluoro-5,6,7,8-tetrahydro-

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Reaction Steps

A solution of 8-(3,4-difluorophenyl)-6-fluoro-[1,2,4]triazolo[1,5-a]pyridin-2-amine (prepared in analogy to example 66a-c starting with 3-bromo-5-fluoropyridin-2-amine, 237 mg, 897 μmol) in ethanol (8 mL) and HCl (25% in water, 144 mg, 120 μL, 987 μmol) was hydrogenated at 80° C. and 80 bar for 18 hours in the presence of Pd/C (237 mg, 222 μmol). The catalyst was filtered off, washed thoroughly with MeOH and the solvents were evaporated. The crude material was purified by flash chromatography (silica gel, 50 g, 0% to 15% MeOH/NH4OH (9:1) in dichloromethane). The title compound was obtained as white foam (76 mg, 32%). MS ISP (m/e): 269.2 (100) [(M+H)+].

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