反应详情

Water (2 ml) is added to a mixture of 3-[5-(1-azido-ethyl)-4-methyl-thiophen-2-yl]-5-(3,5-dichloro-phenyl)-5-trifluoromethyl-4,5-dihydro-isoxazole (0.80 g) and triphenylphosphine (0.93 g) in tetrahydrofuran (9 ml). After 18 hours at 50° C., the reaction mixture is concentrated in vacuo. The crude product is purified on a semi-preparative HPLC to yield 1-{5-[5-(3,5-dichloro-phenyl)-5-trifluoromethyl-4,5-dihydro-isoxazol-3-yl]-3-methyl-thiophen-2-yl}-ethylamine (0.284 g) as an orange solid.

1. concentrationthe reaction mixture is concentrated in vacuo
2. customThe crude product is purified on a semi-preparative HPLC