反应详情

Borane dimethyl sulfide complex (0.73 ml) is added to a solution of 5-[5-(3,5-dichloro-phenyl)-5-trifluoromethyl-4,5-dihydro-isoxazol-3-yl]-2-methyl-thiophene-3-carbonitrile (2.8 g) in THF (21 ml) at reflux. After 30 minutes at reflux, the reaction is cooled down to room temperature. HCl (6.2 ml, 1.25M in MeOH) is added and the reaction mixture is refluxed for 30 minutes. The mixture is then concentrated in vacuo to yield C-{5-[5-(3,5-dichloro-phenyl)-5-trifluoromethyl-4,5-dihydro-isoxazol-3-yl]-2-methyl-thiophen-3-yl}-methylamine as a brown foam (2.9 g). The crude product is used without further purification.

1. temperatureat reflux
2. temperatureAfter 30 minutes at reflux
3. temperaturethe reaction mixture is refluxed for 30 minutes
4. concentrationThe mixture is then concentrated in vacuo