反应详情

To a stirred solution of 6-((2R,3S,4R,5S)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-neopentylpyrrolidine-2-carboxamido)-2-naphthoic acid (58 mg, 0.091 mmol) in methylene chloride (8 ml), HATU (35 mg, 0.091 mmol) was added followed by DIPEA (0.15 ml). The solution was stirred for 5 minutes and then ammonia in methanol (2M in methanol, 1.0 ml) was added and the mixture was stirred at rt for 3 hrs. The solvent was reduced to 4 ml and loaded onto a silica gel column and eluted with 5% Methanol/methylene chloride on a combifalsh machine to give a white solid. 49 mg, 84.5%. (ES+) m/z Calcd: [(M+H)+]: 635. found: 635.

1. stirringthe mixture was stirred at rt for 3 hrs
2. washeluted with 5% Methanol/methylene chloride on a combifalsh machine
3. customto give a white solid