Diversity oriented synthesis: iminium chemistry applied to heterocyclic synthesis and medicinal chemistry

• Grant number: 10/11945-8
• Support Opportunities: Scholarships in Brazil - Scientific Initiation
• Start date: October 01, 2010
• End date: September 30, 2011
• Field of knowledge: Physical Sciences and Mathematics - Chemistry - Organic Chemistry
• Agreement: NSF - American Universities (Chemistry)
• Principal Investigator: Flavio da Silva Emery
• Grantee: Paulo Eliandro da Silva Júnior
• Supervisor: Alan R. Katritzky
• Institution abroad: Virginia Commonwealth University (VCU), United States
• Host Institution: Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP). Universidade de São Paulo (USP). Ribeirão Preto , SP, Brazil

Abstract

Heterocyclic compounds constitutes a large fraction of the chemical space of drugs, however, despite the structural diversity, there are few new skeletons introduced each year and more, acknowledging the success of the cyclical patterns more common, little innovation is made in order to discover new molecules. Recent work showed new structural pattern potentially useful in medicinal chemistry. Exploiting this information, this project aims to synthesize heterocyclic nuclei less explored by the organic synthesis and medicinal chemistry, using an approach that uses the chemistry of iminium ion to several heterocyclics reactions. The feasibility of this methodology is applied to the synthesis of heterocycles with a wide functional diversity to warrant further studies in medicinal chemist. (AU)