One of the major issues facing chemists in the coming century is how to synthesize products such as pharmaceuticals, biomolecules, or advanced materials without the waste, cost and time, that is typically required of traditional synthetic methods. To address this, a thrust of our research is to use metal and related catalysts to develop efficient alternatives to the classic multistep synthesis. Our approach is to consider organic products as arising from multiple simple and/or renewable building blocks assembled together all at once via catalysis: a metal catalyzed multicomponent synthesis. These transformations exploit the reactivity metal catalysts to mediate a series of operations, each of which is controlled by the reaction mechanism, instead of the more traditional use of catalysis in single bond forming steps. We have found this method can be viable, and used to assemble a broad range of products. These reactions display many of the features desired in synthetic processes (single step reactions, atom efficient, minimal waste, ease of synthesis). Because of their synthetic simplicity, they can streamline how we consider constructing pharmaceutically relevant targets, and provide routes to generate and tune new variants of pharmacophore. We are pursuing the application of this approach to synthesize a range of new core structures, the mechanism and design of new transition metal catalysts for these transformations, as well as their use in preparing important biological targets structures to discover their properties.