Production of cyclohexylamine derivatives by reductive amination of cyclohexanone derivatives

摘要

Production of cis 4-substituted cyclohexylamines by reductive amination of cyclohexanones in the presence of hydrogen and optionally an organic solvent comprises reacting a 4-substituted cycloalkanone with benzylamine or alpha -methylbenzylamine in the presence of a nickel or platinum-group metal catalyst and reacting the product in the presence of a platinum-group metal catalyst. Production of cis 4-substituted cyclohexylamines by reductive amination of cyclohexanones in the presence of hydrogen and optionally an organic solvent comprises: (a) reacting a cycloalkanone of formula (I) with a benzylamine of formula (VI) in the presence of a nickel or platinum-group metal catalyst to obtain a N-benzyl-cyclohexylamine of formula (VII); and (b) reacting (VII), optionally after replacing or removing the solvent, in the presence of a platinum-group metal catalyst to obtain a cis 4-substituted cyclohexylamine of formula (II): R = an optionally substituted aliphatic or aromatic group or an alkyl-, alkoxy- and/or phenyl-substituted silyl group; X = H or Me.