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

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

1997-09-18

1998-08-04

Morris, Patricia L.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C07D21102

Patent

active

057895961

ABSTRACT:
1-Acyl-4-arylpiperidines of the general formula: ##STR1## wherein R.sup.1 is an aryl group optionally substituted by one or more C.sub.1-6 -alkyl groups, C.sub.1-6 -alkoxy groups, benzyloxy groups or C.sub.1-6 -alkylthio groups and/or one or more fluorine atoms, and R.sup.2 is a C.sub.1-6 -alkyl group, a C.sub.1-6 -alkoxy group, an optionally substituted aryl group, alkylaryl group or a benzyloxy group optionally substituted on the phenyl radical. The 1-acyl-4-arylpiperidines of formula I 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, neurokinin receptor antagonists.

REFERENCES:
patent: 5374728 (1994-12-01), Kampmann et al.
International Published Application No. WO 95/16682 Jun. 1995.
Gundersen, Lise-Lott, et al., Tetrahedron, vol. 48, No. 27, (1992) pp. 5647 to 5656.
Rosentreter, U., Synthesis, No. 2, (Feb. 1985) pp. 210 to 212.

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