Methylamine → tert-Butyl 4-(methylamino)piperidine-1-carboxylate

Participants

Reaction Steps

To a solution of tert-butyl 4-oxo-1-piperidinecarboxylate (0.50 g, 2.5 mmol, Aldrich) and 2.0 M methylamine in Tetrahydrofuran (10. mL, 20. mmol, Aldrich) was added sodium triacetoxyborohydride (1.3 g, 6.3 mmol). After stirring of the suspension overnight, the reaction was quenched with water and stirred for 1 hour. Brine was added and the product was extracted with two portions of DCM. The combined organic extracts were dried over sodium sulfate, filtered and concentrated. The product was used without further purification in Step 2. LCMS (M+H)+: 215.2.

Provenance & Evidence