Patent ID: 8946433
Filing Date: 2015-02-03
Classification: C07D

Abstract:
1. A process for preparing a compound of Formula (3), the process comprising: (i) contacting a substituted 4-hydroxymethyl-4-aminopiperidine of Formula (2) with a dispersion comprising between about 50 and about 70% by weight (based on the total weight of the dispersion) alkali metal hydride in the presence of an alcohol catalyst and an organic solvent selected from the group consisting of N, N-dimethyl tormamide (DMF), 1methyl-2-pyrrolidinone (NMP), dimethoxy ethane (glyme), diethylene glycol diethyl ether (diglyme), dimethyl sulfoxide (DMSO), and combinations thereof, to deprotonate the hydroxyl group of the substituted 4-hydroxymethyl-4-aminopiperidine; and, (ii) reacting an alkylating agent with the deprotonated, substituted 4-hydroxymethyl-4 aminopiperidine to form the compound of Formula (3).