Dr. Emma Edelstein Will Discuss Synthetic Innovations in Drug Discovery: Development of Methods Toward the Synthesis of Substituted Heterocycles
Join the Department of Chemistry online or virtually as we welcome back Emma Edelstein, PhD, senior scientist at Merck and GW Department of Chemistry alumna. Dr. Edelstein will be discussing synthetic innovation in drug discovery. Emma received her B.S. degree from GW, where she conducted undergraduate research for the Dowd Lab. This event will be hosted online and in-person.
Lengthy cycle times in the discovery of drug candidates, compounded by high levels of attrition as they progress through clinical development, severely hampers efficiency in Pharmaceutical R&D. Excellence in synthetic chemistry has the potential to be a key mitigating factor capable of increasing the probability of success and accelerating programs through all stages of their life cycles, particularly in discovery and early development where synthesis is often on the critical path. As part of this guiding principle, this presentation will describe recent examples of synthetic innovation from the Discovery Process Chemistry group at Merck toward the synthesis of substituted heterocyclic scaffolds. Specifically, a Rh-catalyzed conjugate addition reaction toward the synthesis of trans-3-substituted proline derivatives will be described. A high-throughput experimentation campaign was used to identify an efficient chiral catalyst which was able to afford the desired products in high yield and with high levels of diastereo- and enantioselectivity. This method was used to afford a range of 3-substituted pyrrolidine analogues from readily available dehydroproline-derived electrophiles and boronic acid nucleophiles.