反应详情

Boron tribromide (0.229 mL, 2.42 mmol) was added to a solution of 1-(2,6-dichloropyridin-4-yl)-1-(3-methoxyphenyl)-1H-isoindol-3-amine (Scheme #19, C, 0.62 g, 1.61 mmol) in dry dichloromethane (40 mL) at 0° C. The reaction was aloud to reach room temperature and stirred for 6 h. The reaction was quenched by addition of saturated aqueous sodiumhydrogen carbonate and extracted with dichloromethane. The organic phase was washed with brine, dried over magnesium sulfate and evaporated. Purification by flash chromatography using ethyl acetate afforded 0.302 g (51% yield) of the title compound. 1H NMR (DMSO-d6) δ 7.86-7.77 (m, 2 H), 7.53-7.46 (m, 2 H), 7.37 (s, 2 H), 7.07 (t, J=7.83 Hz, 1 H), 6.96 (br s, 2 H), 6.72-6.58 (m, 3 H); MS (API) m/z 370 [M+1]+.

1. customto reach room temperature
2. customThe reaction was quenched by addition of saturated aqueous sodiumhydrogen carbonate
3. extractionextracted with dichloromethane
4. washThe organic phase was washed with brine
5. dry with materialdried over magnesium sulfate
6. customevaporated
7. customPurification by flash chromatography