Our laboratory is deeply interested in the discovery and development of new reaction methodology en route to the chemical synthesis of complex bioactive molecules. Over the course of many years, research in our group at the California Institute of Technology has been pursued in the general area of synthetic chemistry, with a focus on the development of new strategies for the preparation of complex molecules. Concurrent to this program of target driven synthesis is a strong effort directed toward the development of new catalytic reaction methods, which will be useful for a range of applications. Typically, the complex target structure is used as an inspiration for the discovery of new reactions and technologies that may eventually be regarded as general synthetic methodology. Consequently, this approach provides access to a) novel, medicinally relevant structures, b) a general method for their synthesis, and c) new synthetic methods that will be beneficial for a host of applications. These topics will be discussed in the lecture.