反应详情

温度

0 °C

120 μl (680 μmol) of borane/N,N-diethylaniline complex are added slowly to a solution of 3.79 mg (30 μmol) of (1R,2S)-1-aminoindan-2-ol in 4 ml of tetrahydrofuran. The mixture is then cooled to 0° C., and a solution of 82 mg (170 μmol) of 5-(4-fluorophenyl)-7-isopropyl-2,2-dimethyl-6-[4-(trifluoromethyl)benzoyl]-2,3-dihydro-4H-chromen-4-one (Example 23A) in 4 ml of tetrahydrofuran is then slowly added dropwise. The mixture is allowed to thaw slowly and stirred at room temperature overnight. Methanol is then added, and the solvent is removed under reduced pressure. The residue is taken up in ethyl acetate and washed in each case twice with 1 M hydrochloric acid and saturated sodium bicarbonate solution and once with saturated sodium chloride solution. The organic phase is dried over sodium sulfate and then concentrated under reduced pressure. Purification of the residue by column chromatography on silica gel (mobile phase: gradient cyclohexane→cyclohexane/ethyl acetate 10:1) gives the target compound.

1. customthe solvent is removed under reduced pressure
2. washwashed in each case twice with 1 M hydrochloric acid and saturated sodium bicarbonate solution and once with saturated sodium chloride solution
3. dry with materialThe organic phase is dried over sodium sulfate
4. concentrationconcentrated under reduced pressure
5. customPurification of the residue by column chromatography on silica gel (mobile phase: gradient cyclohexane→cyclohexane/ethyl acetate 10:1)
6. customgives the target compound