反应详情

2-[2-(2-Methyl-propenyl)-3-trifluoromethyl-benzoylamino]-indan-2-carboxylic acid ethyl ester (2) (100 mg, 0.32 mmol) is dissolved in EtOH (20 mL) and set to stir at RT. To this solution is added 5M KOH (2 mL). The reaction mixture is heated to reflux and stirred for 1 h. After concentration in vacuo, the resulting residue is dissolved in water (10 mL) and washed with EtOAc (20 mL). The phases are separated and the aqueous phase is acidified with concentrated HCl to pH 2. The aqueous phase is washed with 50 mL ether (3×). Organic phases are collected, concentrated to dryness, then the resulting residue is purified on an HPLC. The desired product (397) is obtained as white solid (40.0 mg, 43%).

1. temperatureThe reaction mixture is heated
2. temperatureto reflux
3. stirringstirred for 1 h
4. concentrationAfter concentration in vacuo
5. dissolutionthe resulting residue is dissolved in water (10 mL)
6. washwashed with EtOAc (20 mL)
7. customThe phases are separated
8. washThe aqueous phase is washed with 50 mL ether (3×)
9. customOrganic phases are collected
10. concentrationconcentrated to dryness
11. customthe resulting residue is purified on an HPLC