Pharmaceutical alkaloids: The search for an effective smoking cessation treatment

ORGN 36

Jotham W. Coe, coejw@groton.pfizer.com, Neuroscience, Pfizer Global Research and Development, Eastern Point Road, Groton, CT 06340
The synthetic inspiration behind CHANTIX™ (varenicline tartrate), the first FDA approved non-nicotine medicine designed specifically to help smokers quit smoking, will be presented. The emphasis will be on the methods developed to synthesize the natural product cytisine, their extension to novel nicotinic alkaloids, and how the chemistry was ultimately steered to the discovery of varenicline by incorporation of historical benzomorphan structural insights.