Methanesulfonyl chloride → 1-(tert-Butoxycarbonyl)-4-(methanesulfonyloxy)piperidine

Participants

Reaction Steps

At 0° C., to a solution of 4-hydroxy-piperidine-1-carboxylic acid tert-butyl ester (4 g, 20.20 mmol) and DMAP (3 g, 24 mmol) in DCM (50 mL) was added methanesulfonyl chloride (2.7 g, 24 mmol). After stirred for 2 h, the mixture was filtrated. The filtrate was washed by 0.5N HCl (50 mL), Na2CO3 aqueous solution (1 M, 50 mL) and brine (50 mL), dried over anhydrous Na2SO4, and concentrated to give the title compound as a yellow solid (5 g).

Provenance & Evidence