Water → Tert-butyl 4-(methylsulfonyloxymethyl)piperidine-1-carboxylate

Participants

Reaction Steps

Under an argon atmosphere, the tert-butyl-4-hydroxymethylpiperidine-1-carboxylate obtained in Step 1 (12.9 g, crude) was dissolved in anhydrous tetrahydrofuran (100 mL), triethylamine (17 mL, 120 mmol) was added, thereafter methanesulfonyl chloride (3.5 mL, 44 mmol) was added dropwise under ice-cooling over about 10 minutes, and stirring was further conducted under ice-cooling for 30 minutes. Water was added to the reaction liquid to quench the reaction, and the reaction liquid was extracted with ethyl acetate. The organic layer was dried over anhydrous sodium sulfate and concentrated under a reduced pressure to give tert-butyl-4-{[(methylsulfonyl)oxy]methyl}piperidine-1-carboxylate (15.3 g) as a crude purified product.

Provenance & Evidence