反应详情

温度

23 °C

To a solution of (S)-1-{(S)-2-[(S)-2-(tert-butoxycarbonyl-methyl-amino)-propionylamino]-2-phenyl-acetyl}-2,3-dihydro-1H-indole-2-carboxylic acid ethyl ester (2.28 g, 4.47 mmol, Eq: 1) in 60 mL of THF/water/MeOH (3:1:1) was added 1 M aqueous lithium hydroxide (13.4 mL, 13.4 mmol, Eq: 3). The reaction mixture was stirred at 23° C. for 2.5 h. The reaction was concentrated in vacuo and the residue was taken up in water and acidified with 6 M and then 1 M aqueous HCl to pH˜2. The mixture was extracted with EtOAc (2×50 mL) and the organic layers were combined, dried over Na2SO4 and concentrated in vacuo to afford (S)-1-{(S)-2-[(S)-2-(tert-butoxycarbonyl-methyl-amino)-propionylamino]-2-phenyl-acetyl}-2,3-dihydro-1H-indole-2-carboxylic acid as a white foam (2.04 g), m/z=482 (M+H).

1. concentrationThe reaction was concentrated in vacuo
2. extractionThe mixture was extracted with EtOAc (2×50 mL)
3. dry with materialdried over Na2SO4
4. concentrationconcentrated in vacuo