Process for the preparation of 1-acyl-4-arylpiperidines

C - Chemistry – Metallurgy – 07 – D

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C07D 211/18 (2006.01) C07D 211/16 (2006.01) C07D 211/20 (2006.01) C07D 211/90 (2006.01)

Patent

CA 2214288

1-Acyl-4-arylpiperidines of the general formula: (see formula I) wherein R1 is an aryl group optionally substituted by one or more C1-6-alkyl groups, C1-6-alkoxy groups, benzyloxy groups or C1-6-alkylthio groups and/or one or more fluorine atoms, and R2 is a C1-6-alkyl group, a C1-6-alkoxy group, an optionally substituted aryl group, alkylaryl group or a benzyloxy group optionally substituted on the phenyl radical, are prepared by reacting an arylmagnesium halide with a 1-acylpyridinium halide, obtainable from pyridine and an acyl halide, in the presence of a copper compound to give the corresponding 1-acyl-4-aryl-1,4-dihydropyridine, and hydrogenating the latter. The 1-acyl-4-arylpiperidines are intermediates in the synthesis of pharmaceutical active ingredients, for example, of neurokinin receptor antagonists.

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