tert-butyl (1-(2,2,2-trifluoroethyl)piperidin-4-yl)carbaMate synthesis

Yield:335653-59-3 94.7%

Reaction Conditions:

with triethylamine in tetrahydrofuran at 75; for 16 h;

Steps:

127.1 The first step: preparation of tert-butyl (1-(2,2,2-trifluoroethyl)piperidin-4-yl)carbamate:

4-Boc-aminopiperidine (200mg, 1.00mmol, 1.0eq), triethylamine (404mg, 3.99mmol, 4.0eq) were dissolved in tetrahydrofuran (2.5mL),Then 2,2,2-trifluoroethyl trifluoromethanesulfonate (278 mg, 1.20 mmol, 1.2 eq) was added, and the mixture was reacted at 75° C. for 16 hours. The reaction solution was concentrated, and the crude product was separated and purified by flash chromatography (silica gel, DCM:MeOH=15:1) to obtain the title compound (267 mg, 94.7%) as a white solid.

References:

WO2022/48631,2022,A1 Location in patent:Page/Page column 153-154