| 摘要 |
The present invention relates to a novel process for the preparation of N-heterocyclealkanamide derivatives having the following formula: <IMAGE> (I) which comprises reacting 1-(2-chloroethyl)piperidine with 2-chlorobenzeneacetonitrile to give (+/-)- alpha -(2-chlorophenyl)-1-piperidinebutanenitrile; alkylating the piperidenebutanenitrile to give (+/-)- alpha -(2-chlorophenyl)- alpha -(2,2-dimethoxyethyl)piperidine-1-butanenitrile; hydrolyzing the resulting alkylated piperidinebutanenitrile to give (+/-)- alpha -(2-chlorophenyl)- alpha -(2-oxoethyl)piperidine-1-butanenitrile; reacting the resulting piperidinebutanenitrile with isopropylamine to form (+/-)- alpha -(2-chlorophenyl)- alpha -[2-[(1-methylethyl)imino]ethyl]piperidine-1-butanenitrile; reducing the resulting imine to form (+/-)- alpha -(2-chlorophenyl)- alpha -[2-[(1-methylethyl)amino]ethyl]-piperidine-1-butanenitrile; acetylating the resulting amine to form (+/-)-N-[3-(2-chlorophenyl)-3-cyano-5-(1-piperidinyl)pentyl]-N-(1-methylethyl)acetamide; hydrolyzing the resulting acetylated amino substituted piperidine butanenitrile to form (+/-)- alpha -[2-[acetyl(1-methylethyl)amino]ethyl]- alpha -(2-chlorophenyl)-1-piperidinebutanamide; and isolating the resulting piperidinebutanamide.
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