反应详情

To 2-(2-(6-((R)-1-((S)-3-(tert-butoxycarbonylamino)pyrrolidin-1-yl)-2,2,2-trifluoroethyl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)-6-fluoro quinolin-7-yloxy)ethyl acetate (250 mg, 0.395 mmol) (Example 122, Step A) in MeOH (5 mL) was added 2N LiOH (1 mL) and the reaction was stirred at ambient temperature for 1 hour. The reaction was concentrated and the residue purified by reverse phase chromatography (SP4, 12M, eluting with a gradient of water/ACN 100:0 to 0:100, 25 column volumes) to yield tert-butyl (S)-1-((R)-2,2,2-trifluoro-1-(3-(6-fluoro-7-(2-hydroxyethoxy)quinolin-2-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yl)ethyl)pyrrolidin-3-ylcarbamate (210 mg, 90.0% yield) as a white solid.

1. concentrationThe reaction was concentrated
2. customthe residue purified by reverse phase chromatography (SP4, 12M
3. washeluting with a gradient of water/ACN 100:0 to 0:100, 25 column volumes)