Late Stage Functionalization (LSF) holds the potential to revolutionize the logic of chemical synthesis and open new ways to prepare novel natural products and medicines. The introduction of important chemical groups for medicinal chemistry in the very last steps of the synthesis through LSF could also dramatically speed up the preparation of NCEs and have a major impact on drug discovery. The availability of new powerful catalytic chemistries showing a high degree of functional group tolerance and that can be performed under mild conditions offer tremendous opportunities for chemists to access new molecules that cannot be made easily by conventional approaches.