反应详情

4.4 g crude 2-Chloro-N-hydroxy-4-{4-methyl-2-[2-(4-trifluoromethyl-phenyl)-ethyl]-oxazol-5-ylmethoxy}-benzamidine were dissolved in 20 ml dichloromethane. 0.94 ml pyridine and 1.46 ml phenylchloroformate were added and the mixture stirred at room temperature for ten minutes. The mixture was diluted by the addition of 40 ml acetonitrile and 7.25 ml 1,8-diazabicyclo[5.4.0]undec-7-ene were added. The mixture was stirred at room temperature for 10 minutes. The mixture was evaporated in vacuo and the resulting crude material was purified by reversed phase HPLC to obtain 460 mg 3-(2-chloro-4-{4-methyl-2-[2-(4-trifluoromethyl-phenyl)-ethyl]-oxazol-5-ylmethoxy}-phenyl)-4H-[1,2,4]oxadiazol-5-one.

1. additionwere added
2. stirringThe mixture was stirred at room temperature for 10 minutes
3. customThe mixture was evaporated in vacuo
4. customthe resulting crude material was purified by reversed phase HPLC