The ability to prepare highly functionalized molecules in general and predictable ways is central to modern drug design and discovering new treatments for human disease. The aim of our program is to create new methods to solve the longstanding synthetic challenge of asymmetrically constructing biologically active small molecules. Classical synthetic approaches based on CH activations are ubiquitous but limited by the inherent directing effects of embedded heteroatoms. This presentation will discuss our recently discovered scheme to access highly basic ion pairs with organolithiums which provides a new pathway to override intrinsic heteroatom directing effects. In addition, we will describe our progress in developing new methods for carbon-oxygen bond formation reactions that utilizes primary ozonide intermediates.