| 摘要 |
A process for the production of Sibutramine i.e. N-1-[1-(4-chlorophenyl) cyclobutyl]-3-methylbutyl-N, N-dimethylamine of formula (I) comprising the steps of: (a) reacting a nitrile, 1-(4-chlorophenyl) cyclobutyl carbonitrile of formula (III) with a Grignard reagent, namely isobutyl magnesium bromide to produce the magnesium complex of formula (IV); (b) cleaving the magnesium complex of formula (IV) under basic conditions to form an imine of formula (VIII); (c) reducing the imine of formula (VIII) by a metal hydride to obtain an amine of the formula (VII), and (d) converting the amine (VII) first to its hydrochloride and then to Sibutramine of formula (I) by Eschweiler Clarke methylation. |
