Methanesulfonic Acid → HCID 49833441, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of 7-(3-(tert-butoxycarbonylamino)pyrrolidin-1-yl)-6-(6-(3-ethylureido)-4-(4-(trifluoromethyl)thiazol-2-yl)pyridin-3-yl)-1-((S)-1-hydroxy-3,3-dimethylbutan-2-yl)-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid (Intermediate 105) (290 mg, 0.37 mmol, 1 equiv.) in dichloromethane (2 mL) was added methanesulfonic acid (0.048 mL, 0.73 mmol, 2 equiv.). The reaction was stirred at 23° C. for 2 h. The reaction was concentrated and re-suspended in water. The precipitate was discarded, and the filtrate was concentrated. The compound was purified via C18 silica gel chromatography and concentrated to afford 7-(3-aminopyrrolidin-1-yl)-6-(6-(3-ethylureido)-4-(4-(trifluoromethyl)thiazol-2-yl)pyridin-3-yl)-1-((5)-1-hydroxy-3,3-dimethylbutan-2-yl)-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid (28.7 mg, 11%).

Provenance & Evidence