Targeting Type 2 diabetes, a highly potent and selective imidazolone-based glucagon receptor antagonist, SCH 900822, has been discovered. We will illustrate the synthesis and structure-activity relationships of the series as well as the pharmacokinetic and biologic results. During the exploration of the imidazolone core, novel formal olefination and acylaziridination of imidazolones were obtained by cycloaddition of cyclic nitrones with alkenes and alkynes, repectively. The mechanisms and scopes of these two reactions will be briefly discussed.

Example of drug discovery program leading to the development of novel reactions

244th National Meeting (2012)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.