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N-Methyl-1-(phenylmethyl)-3-piperidinamine synthesis

3synthesis methods
-

Yield:-

Reaction Conditions:

with sodium tris(acetoxy)borohydride in tetrahydrofuran;dichloromethane at 20;

Steps:

24.1 Step 1: 1-benzyl-N-methylpiperidin-3-amine

To a solution of 1-benzylpiperidin-3-one (1.0 g, 5.3 mmol) in dichloromethane (25 mL) was added a solution of methylamine in tetrahydrofuran (5.3 mL, 2 M, 10.6 mmol). The mixture was stirred at room temperature for 5 minutes then NaBH(OAc)3 (2.2 g, 10.6 mmol) was added to the solution. The mixture was stirred at room temperature overnight then washed with saturated aqueous NaHCO3 solution, dried and concentrated under vacuum to give 1- benzyl-N-methylpiperidin-3-amine (1.0 g, crude). LCMS m/z = 205.1 [M+H]+.

References:

WO2017/216726,2017,A1 Location in patent:Page/Page column 565