反应详情

4-[7-Chloro-1-oxo-2-(4-trifluoromethoxybenzyl)-2,3-dihydro-1H-isoindol-5-ylmethyl]-piperidine-1-carboxylic acid tert-butyl ester (54.90 mg, 0.102 mmol) was stirred in dichloromethane (2 mL) and trifluoroacetic acid (2 mL) overnight. The reaction mixture was quenched with sodium carbonate to pH=8-9 and the free base was extracted with dichloromethane. The organic layer was washed with water, brine, dried over sodium sulfate, filtered and concentrated to provide the title compound (48.9 mg, 100%). 1H NMR (300 MHz, CDCl3): δ 7.39 (d, 2H), 7.18 (d, 3H), 7.06 (s, 1H), 4.77 (s, 2H), 4.61 (broad s, 1H), 4.23 (s, 2H), 3.16 (d, 2H), 2.62 (m, 4H), 1.61 (d, 3H), 1.29 (m, 2H).

1. customThe reaction mixture was quenched with sodium carbonate to pH=8-9
2. extractionthe free base was extracted with dichloromethane
3. washThe organic layer was washed with water, brine
4. dry with materialdried over sodium sulfate
5. filtrationfiltered
6. concentrationconcentrated