Tert-butyl 4-(hydroxymethyl)piperidine-1-carboxylate → tert-Butyl 4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]oxy}methyl)piperidine-1-carboxylate

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Reaction Conditions

Reaction Steps

A mixture of 4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-ol (0.12 g, 0.50 mmol, EXAMPLE 1, step 2), tert-butyl 4-(hydroxymethyl)piperidine-1-carboxylate (0.13 g, 0.60 mmol), and dimethyl (tributylphosphoranylidene)malonate (0.32 g, 1.0 mmol, J. Org. Chem. 2003, 68, 1597-1600) in toluene (0.5 mL) was stirred at 80° C. for 16 h. The mixture was purified by silica gel column chromatography (hexane/ethyl acetate 4:1) to give 0.14 g (65%) of the title compound as a white solid.

Provenance & Evidence