Synthesis of substituted azaindoles and their lead-like libraries

ORGN 795

Garry R. Smith, Michael W. Wagaman, and Alan E. Blize. Department of Chemistry, ASDI, Inc, 601 Interchange Blvd., Newark, DE 19711
Recent popularity aside, azaindoles have been under-represented in drug discovery research. While these compounds have clear physiochemical advantages versus indoles, they have suffered due to a lack of commercially available representatives. We have been exploring the synthesis of all azaindole isomers, and related compounds, bearing varied substitution patterns useful for drug discovery. These studies have led to the discovery of new routes to these compounds and the production of compounds bearing useful functional groups in unusual substitution patterns. From these compounds, we have prepared diverse lead-like libraries for high throughput screening studies. The design of these libraries provides libraries that are diverse, yet with sufficient similarity built in to allow immediate confirmation of any hits. The poster will present the design of these libraries as well as challenges encountered during synthesis and purification.