反应详情

温度

100 °C

A mixture of 4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-ol (230 mg, 1 mmol, EXAMPLE 1, step 2), methyl 4-{[4-(hydroxymethyl)piperidin-1-yl]methyl}tetrahydro-2H-pyran-4-carboxylate (270 mg, 1 mmol, EXAMPLE 1, step 4), and cyanomethyltributylphosphorane (400 mg, 1.5 mmol) in toluene (1.0 mL) was stirred at 100° C. for 16 h. After cooling, the mixture was concentrated in vacuo to give a dark brown oil. The residual oil was purified by silica gel column chromatography (hexane/ethyl acetate 2:1) to give 250 mg (51%) of the title compound as a white solid.

1. temperatureAfter cooling
2. concentrationthe mixture was concentrated in vacuo
3. customto give a dark brown oil
4. customThe residual oil was purified by silica gel column chromatography (hexane/ethyl acetate 2:1)