反应详情

To solution of 3,3-difluoro-4-[8-(2,3,4-trifluoro-phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-ylamino]-piperidine-1-carboxylic acid tert-butyl ester (110 mg, 228 μmol) in CH2Cl2 (4 mL) at 0° C. was added TFA (182 mg, 123 μl, 1.59 mmol) and stirred at room temperature for 18 hours. Further TFA (182 mg, 123 μl, 1.59 mmol) was added and stirred at 50° C. for 6 hours. The reaction mixture was extracted with saturated NaHCO3 solution and ethyl acetate, the organic layers combined, dried over Na2SO4, filtered and the solvents evaporated. The product was coevaporated four times with toluene. The title compound was obtained as light yellow foam (87 mg, 100%). MS ISP (m/e): 384.2 (100) [(M+H)+].

1. stirringstirred at 50° C. for 6 hours
2. extractionThe reaction mixture was extracted with saturated NaHCO3 solution and ethyl acetate
3. dry with materialdried over Na2SO4
4. filtrationfiltered
5. customthe solvents evaporated