反应详情

40 μl (210 μmol) of borane/N,N-diethylaniline complex are added slowly to a solution of 1.2 mg (10 μmol) of (1R,2S)-1-aminoindan-2-ol in 1.5 ml of tetrahydrofuran, and the mixture is stirred for 30 min. A solution of 23 mg (50 μmol) of 5-cyclopentyl-7-isopropyl-2,2-dimethyl-6-[4-(trifluoromethyl)benzyl]-2,3-dihydro-4H-chromen-4-one (Example 39A) in 1.5 ml of tetrahydrofuran is then added very slowly dropwise, and the mixture is stirred for 2 h. Methanol is then added, and the mixture is concentrated 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) gives the target product.

1. stirringthe mixture is stirred for 2 h
2. concentrationthe mixture is concentrated under reduced pressure
3. washwashed in each case twice with 1 M hydrochloric acid and saturated sodium bicarbonate solution and once with saturated sodium chloride solution
4. dry with materialThe organic phase is dried over sodium sulfate
5. concentrationconcentrated under reduced pressure
6. customPurification of the residue by preparative HPLC (method 1)
7. customgives the target product