Triphenylphosphine → 1-Piperidinecarboxylic acid, 4-[3-(trifluoromethyl)-1H-pyrazol-1-yl]-, 1,1-dimethylethyl ester

Participants

Reaction Steps

To a tetrahydrofuran solution (1.0 mL) of 3-(trifluoromethyl)-1H-pyrazole (272 mg, 2.00 mmol), tert-butyl 4-hydroxy-piperidine-1-carboxylate (402 mg, 2.00 mmol), and triphenylphosphine (629 mg, 2.40 mmol), diisopropyl azodicarboxylate (1.36 mL, 2.60 mmol, toluene solution) was added at room temperature and the resultant solution was stirred at room temperature for 22 hours. After completion of the reaction, the reaction solution was concentrated under reduced pressure and purified by preparative liquid chromatography to obtain the title compound (289 mg, yield 45%).

Provenance & Evidence