反应详情

To a solution of 4-{2-[(3-bromo-4-chloro-benzoyl)-methyl-amino]-phenyl}-butyric acid methyl ester (1.11 g, 2.6 mmol, Step 13D) in THF (8 mL), 2N LiOH (6.5 mL) was added and the mixture was stirred for 2 hours at it. 1N HCl was added to the reaction mixture to yield a pH ˜2 followed by extraction with EtOAc (2×). The combined organic layers were washed with water and brine, dried (Na2SO4) and concentrated in vacuo to afford 1.1 g of 4-{2-[(3-bromo-4-chloro-benzoyl)-methyl-amino]-phenyl}-butyric acid as a white solid. MS [M+H]+: 411.7; tR=2.57 min, (method 1)

1. customto yield a pH ˜2
2. extractionfollowed by extraction with EtOAc (2×)
3. washThe combined organic layers were washed with water and brine
4. dry with materialdried (Na2SO4)
5. concentrationconcentrated in vacuo