反应详情

温度

0 °C

78 μl (540 μmol) of borane/N,N-diethylaniline complex are added slowly to a solution of 2.46 mg (20 μmol) of (1R,2S)-1-aminoindan-2-ol in 2 ml of tetrahydrofuran. The mixture is then cooled to 0° C., and a solution of 52 mg (110 μmol) of 6-(4-tert-butylbenzoyl)-5-(4-fluorophenyl)-7-isopropyl-2,2-dimethyl-2,3-dihydro-4H-chromen-4-one (Example 29A) in 3 ml of tetrahydrofuran are slowly added dropwise. The mixture is then 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 preparative HPLC (method 1) and subsequent chiral HPLC (method 2) 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 preparative HPLC (method 1) and subsequent chiral HPLC (method 2)
6. customgives the target compound