反应详情

Trifluoroacetic anhydride (26 μL) is added to a solution of 4-[5-(2-fluoro-4-aminocarbonyl-phenyl)-furo[2,3-c]pyridin-2-yl]-piperidine-1-carboxylic acid tert-butyl ester (40 mg) and triethylamine (51 μL) in dichloromethane (3 mL) at room temperature. The solution is stirred at room temperature for 2 h before another portion of trifluoroacetic anhydride (26 μL) and triethylamine (51 μL) is added. The solution is stirred for 0.5 h and then aqueous NaHCO3 solution is added. The resulting mixture is extracted with dichloromethane and the combined extracts are washed with brine, dried (Na2SO4), and concentrated. The residue is triturated with ether and then with methanol to give the title compound. LC (method 3): tR=1.52 min; Mass spectrum (ESI+): m/z=422 [M+H]+.

1. additionis added
2. extractionThe resulting mixture is extracted with dichloromethane
3. washthe combined extracts are washed with brine
4. dry with materialdried (Na2SO4)
5. concentrationconcentrated
6. customThe residue is triturated with ether