反应详情

To a suspension of N-[1-(4-cyanophenyl)cyclopropyl]-2,5-dimethyl-4-[4-(trifluoromethyl)benzyl]thiophene-3-carboxamide from Example 14, Step 2 (174 mg, 0.383 mmol) in toluene (2.5 mL), was added azidotributyltin (317 μL, 1.15 mmol) and the mixture was heated at the reflux temperature. After 20 h, the solution then obtained was allowed to cool to r.t. and AcOH (365 μL) was added. The heterogeneous mixture was stirred for 4 h and the precipitated solid was collected by filtration, successively rinsed with toluene and hexane then dried to afford the desired product as an off-white solid. MS (−APCI): m/z 496 (M−1)−.

1. temperaturethe mixture was heated at the reflux temperature
2. customthe solution then obtained
3. filtrationthe precipitated solid was collected by filtration
4. washsuccessively rinsed with toluene and hexane
5. customthen dried