反应详情

To a stirred solution of methyl 4-((2R,3S,4R,5S)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-neopentylpyrrolidine-2-carboxamido)-2,5-difluorobenzoate (75 mg, 0.118 mmol) in methylene chloride (10 ml), AlBr3 (Aldrich, 59 mg, 0.94 mmol) was added followed by dimethyl sulfide (Aldrich, 0.2 ml, 0.63 mmol). The mixture was stirred at rt for 2 hrs. The solvent was removed and the residue was treated with 3 ml of acetonitrile and 10 ml of water. The mixture was then extracted with ethyl acetate. Removal of solvent gave an off white solid. 72 mg. (ES+) m/z Calcd: [(M+H)+]: 622. found: 622.

1. customThe solvent was removed
2. additionthe residue was treated with 3 ml of acetonitrile and 10 ml of water
3. extractionThe mixture was then extracted with ethyl acetate
4. customRemoval of solvent
5. customgave an off white solid