Synthesis and Preliminary Biological Studies of 3-Substituted Indoles Accessed by a Palladium-Catalyzed Enantioselective Alkene Difunctionalization Reaction

摘要

The indole framework represents a "privileged" structural motif commonly found in pharmaceutical drugs and natural products. Therefore, new methods for accessing unique indole derivatives is of importance for drug lead synthesis. For this reason, we became interested in using indoles as nucleophiles in the enantioselective alkene difunctionalization reactions recently disclosed by our laboratory. Herein we report the successful development of such a reaction and preliminary biological studies showcasing both the activity toward breast cancer cell lines and differential phenotypes for two related derivatives.