Functional group transformation: An efficacy-enhancing approach in combinatorial chemistry

In combinatorial chemistry, the time-consuming step is optimizing the react ion conditions rather than the actual preparation of the library. We propos e a new combinatorial strategy, "functional group transformation", which pe rmits construction of new libraries while making use of much of the chemist ry developed for earlier ones. We use some of our current methods for deter mining chemical diversity to demonstrate that the added diversity of such a transformed library can be as large as that of a library based on totally new chemistry.