Despite centuries of innovation, chemistry is often still the limiting factor in the development of small molecule drug candidates, molecular probes, or novel chemical libraries. Many molecules that have tremendous biological potential are challenging to modify with known chemical methodologies. The overarching goal of our program is to develop robust methods for the synthesis of molecules that have previously been inaccessible. By developing modular, building block strategies for synthesis, we are able to generate libraries of molecules across a broad latitude of molecular classes with unprecedented structural diversity. By design, our research provides opportunities for substantive collaboration with colleagues in adjacent fields, enabled by the interdisciplinary environment at University of California, San Francisco.