反应详情

A solution of (S)-3-t-butoxycarbonylamino-(R)-2-benzyloxy-4-cyclohexylbutyraldehyde (600 mg.) and isobutylammonium p-toluenesulfonate (510 mg.) were stirred together in methanol for 30 minutes at 20° C. and then treated in one portion with sodium cyanoborohydride (105 mg.). After 45 minutes 28 mg. more sodium cyanoborohydride was added and 30 minutes later the mixture was filtered through Celite, concentrated, the residue dissolved in ethyl acetate which was washed twice with aqueous bicarbonate, brine and dried over sodium sulfate. After solvent removal 600 mg. (87%) of the title amine was obtained which was used without additional purification.

1. filtrationwas filtered through Celite
2. concentrationconcentrated
3. dissolutionthe residue dissolved in ethyl acetate which
4. washwas washed twice with aqueous bicarbonate, brine
5. dry with materialdried over sodium sulfate
6. customAfter solvent removal 600 mg