Yield:892493-65-1 84 %

Reaction Conditions:

with dmap in water;acetonitrile at 60; under 3000.3 Torr;Autoclave;Inert atmosphere;Pressure;Reagent/catalyst;Solvent;Temperature;

Steps:

1-5

Add 4-piperidine formic acid hydrochloride (1kg), acetonitrile (2kg), water (1kg), Boc anhydride (1.4kg), 4-dimethylaminopyridine (40g) in 10L autoclave, pass into nitrogen , maintain the pressure of the reaction system at 0.4MPa, react at 60°C for 2h, cool to room temperature 20-25°C, return to normal pressure, continue to cool down to 5-10°C, precipitate solid, filter, and wash the filter cake with ethyl acetate (3kg) for 1 hours, filtered and dried to obtain a white solid with a yield of 84% and a purity of 99%.

References:

CN115322143,2022,A Location in patent:Paragraph 0012; 0021; 0023-0024; 0026-0027; 0029-0030; ...