Elaboration of FragLites via Suzuki-Miyaura Cross-Coupling of 3-D Bifunctional Cyclopropyl-Fused Building Blocks

Fragment-based drug discovery is a common method for the discovery of lead compounds in medicinal chemistry groups both in academia and in the pharmaceutical industry. The research described in this thesis focuses on an investigation of Suzuki-Miyaura cross-coupling reactions using 3-D building block exo-A with FragLites or protected/masked FragLites. A comparison of cross-coupling results obtained between exo-A protected FragLites and their unprotected analogues are summarised below. This clearly demonstrates the efficacy of the protection strategy in facilitating efficient cross-coupling reactions. In addition, some examples of N-functionalisation (after Boc group removal) and deprotection reactions are also described.