| 摘要 |
<p>The present invention relates to a novel process for the preparation of heterocyclic alkylamide derivatives having formula (I), and the pharmaceutically acceptable acid addition salt thereof wherein X represents halo, alkyl having 1 to 6 carbon atoms, hydrido, trifluoromethyl, phenyl, or lower alkoxy having 1 to 6 carbon atoms; Y represents the group -CN or -CONH2; R2 represents alkyl having 1 to 6 carbon atoms; R3 represents acetyl, benzoyl, phenacetyl or trifluoroacetyl; m is the integer 1 to 2 and n is an integer from 1 to 3 inclusive; which comprises alkylating an amionalkanol using a benzaldehyde/aminoalkanol/ketone mixture in the presence of a platinum catalyst to give an alkyl substituted phenylmethylaminoalkanol; halogenating said alkanol using a halogenating agent to give a haloalkyl alkylbenzenemethanamine salt; treating said salt with substituted phenyl piperidinealkanenitrile or substituted phenyl pyrrolidinealkanenitrile in the presence of base and dimethyl sulfoxide to give a substituted phenyl substituted aminoalkyl piperidinealkanenitrile or substituted aminoalkyl pyrrolidinealkanenitrile; hydration of the nitrile to give the corresponding amide; and N-debensylation of the amide followed by acetylation to give the compounds of formula (I) wherein Y is -CONH2.</p> |
