反应详情

Methyl chloroformate (11 μL) is added to a solution of {(S)-6-[(R)-4-piperazin-1-ylmethyl-5-trifluoromethyl-indan-1-yloxy]-2,3-dihydro-benzofuran-3-yl}-acetic acid methyl ester (60 mg) and triethylamine (68 μL) in dichloromethane (2 mL) chilled in an ice bath. The cooling bath is removed and the solution is stirred at room temperature for 2 h. Water is added and the resulting mixture is extracted with dichloromethane. The combined extracts are washed with brine and dried (Na2SO4). The solvent is evaporated and the residue is chromatographed on reversed phase (HPLC; acetonitrile/water) to give the title compound. LC (method 4): tR=0.99 min; Mass spectrum (ESI+): m/z=549 [M+H]+.

1. temperaturechilled in an ice bath
2. customThe cooling bath is removed
3. additionWater is added
4. extractionthe resulting mixture is extracted with dichloromethane
5. washThe combined extracts are washed with brine
6. dry with materialdried (Na2SO4)
7. customThe solvent is evaporated
8. customthe residue is chromatographed on reversed phase (HPLC; acetonitrile/water)