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General procedure for the synthesis of 1-methanesulfonyl-4-tert-butoxycarbonylaminopiperidine from methanesulfonyl chloride and 4-tert-butoxycarbonylaminopiperidine: 5.00 g (25.0 mmol) of Boc-4-aminopiperidine was dissolved in 19.8 mL of pyridine and cooled in an ice bath. 2.13 mL (27.5 mmol) of methanesulfonyl chloride was added slowly and dropwise. The reaction mixture was stirred at room temperature for 16 hours. After completion of the reaction, the reaction mixture was diluted with water and then extracted with dichloromethane (DCM). The organic layer was washed with water, dried over anhydrous magnesium sulfate (MgSO4) and filtered. The solvent was removed by concentration under reduced pressure to give 6.30 g of tert-butyl 1-methanesulfonyl-piperidin-4-yl-carbamate. The yield was 91%; ESI-MS: 279 [M + H]+.

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