Intermediates useful for the preparation of antihistaminic piperidine derivatives

US6147216A · kind A · utility

Assignee

• Merrell Pharmaceuticals, Inc. · US

Inventors

• Richard C. Krauss · Midland, US
• Robert M. Strom · Midland, US
• Carey L. Scortichini · Midland, US
• William J. Kruper, Jr. · Sanford, US
• Richard A. Wolf · Midland, US
• Weishi Wu · Landenberg, US
• Albert A. Carr · Cincinnati, US
• David A. Hay · Indianapolis, US
• Duane E. Rudisill · Sharonville, US
• Gianbattista Panzone · Cornaredo, IT

Key dates

• Filing date: Jun 2, 1995
• Grant date: Nov 14, 2000
• Expiry date: Jun 2, 2015

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C2601/02
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula ##STR1## wherein W represents --C(.dbd.O)-- or --CH(OH)--; PA1 R.sub.1 represents hydrogen or hydroxy; PA1 R.sub.2 represents hydrogen; PA1 R.sub.1 and R.sub.2 taken together form a second bond between the carbon atoms bearing R.sub.1 and R.sub.2 ; PA1 n is an integer of from 1 to 5; PA1 m is an integer 0 or 1; PA1 R.sub.3 is --COOH or --COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; and PA1 pharmaceutically acceptable salts and individual optical isomers thereof, PA1 with the proviso that where R.sub.1 and R.sub.2 are ta to form a second bond between the carbon R.sub.1 and R.sub.2 or where R.sub.1 represented hydroxy integer 0.