The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Aug. 04, 1998

Filed:

Sep. 18, 1997
Applicant:
Inventors:

Walter Brieden, Glis, CH;

Didier Loetscher, Leuk-Stadt, CH;

Andrew Naughton, Visp, CH;

Assignee:

Lonza AG, Valais, CH;

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D / ;
U.S. Cl.
CPC ...
546185 ;
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.


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Brieden, Walter. (1998). Process for the preparation of 1-acyl-4-arylpiperidines (U.S. Patent No. 5789596). U.S. Patent and Trademark Office. https://idiyas.com/patent/badge/5789596

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