反应详情

A solution of methyl (2S,3R,5E)-3-({[(1S)-2,2-dimethyl-1-({[(1R)-1-phenylethyl]amino}carbonyl)propyl]amino}carbonyl)-2-ethoxy-6-(3-fluoro-4-phenoxyphenyl)hex-5-enoate (350 mg, 0.566 mmol) in ethanol (15 mL) was hydrogenated over 10% palladium on charcoal (60 mg) at 3 bar and 20° C. for 16 h. The mixture was filtered through Arbocel filter aid and concentrated under reduced pressure. The residue was dissolved in cyclohexane and evaporated (twice) to give methyl (2S,3R)-3-({[(1S)-2,2-dimethyl-1-({[(1R)-1-phenylethyl]amino}carbonyl)propyl]amino}carbonyl)-2-ethoxy-6-(3-fluoro-4-phenoxyphenyl)hexanoate (368 gm, 105%), as a colourless foam, which was taken onto the next step without purification.

1. filtrationThe mixture was filtered through Arbocel
2. filtrationfilter aid
3. concentrationconcentrated under reduced pressure
4. dissolutionThe residue was dissolved in cyclohexane
5. customevaporated (twice)