反应详情

To a solution of (2S,3R)-3-[(1-cyano-4-hydroxy-7-phenoxy-isoquinoline-3-carbonyl)-amino]-2-methyl-butyric acid tert-butyl ester (32 mg, 0.069 mmol) in CH2Cl2 (3 mL) was added trifluoroacetic acid (2 mL) at 0° C., and the mixture was stirred at r.t. for 2 h. The mixture was concentrated in vacuo, and the resulting residue was dissolved in saturated NaHCO3 and washed several times with ether. The aqueous layer was acidified to pH ˜2 with 4 M HCl, and the resulting precipitate was isolated by filtration to give 24 mg of the title compound as a pale pink solid. MS: (−) m/z 404.32 (M−1).

1. concentrationThe mixture was concentrated in vacuo
2. dissolutionthe resulting residue was dissolved in saturated NaHCO3
3. washwashed several times with ether
4. customthe resulting precipitate was isolated by filtration