|
|
Article: Convenient preparation of aryl-substituted nortropanes by Suzuki-Miyaura methodology (1).
- Article from:
- Canadian Journal of Chemistry
- Article date:
- April 1, 2006
- Author:
CopyrightCOPYRIGHT 2006 NRC Research Press. This material is published under license from the publisher through the Gale Group, Farmington Hills, Michigan. All inquiries regarding rights should be directed to the Gale Group. (Hide copyright information)
|
Introduction
Phenyl piperidines have proven to be valuable templates for the construction of modulators of G-protein coupled receptors (GPCRs), which are the target of the largest group of marketed drugs (~50%). Of the 38 GPCR-targeted drugs on the market, listed in a recent review (1), five are aryl piperidines (Allegra, Claritin, Duragesic, Risperdal) or aryl-substituted bicyclic piperidines (Atrovent, Combivent). Several others are aryl piperazines or morphine-related polycyclic aryl piperidines. To illustrate the structural diversity of piperidine-containing GPCR ligands, some examples are illustrated in the following: [mu]-opioid agonist loperamide (1) (2), ...