New SPECT imaging agents for the translocator protein

Abstract

During the course of the studies outlined in this thesis, a new short and efficient synthesis of PK11195 was developed using Pd(0)-mediated reactions to effect the key carbon-carbon bond forming reactions. PK11195 is a ligand that interacts with the translocator protein(TSPO) in the brain. During brain injury the concentration of TSPO increases, making TSPO an ideal and sensitive biomarker. Using single photon emission computed tomography along with [123I]PK11195, medical practitioners are able to visualize the receptor. In addition to the synthesis of PK11195, three other analogues were devised using the same methodology as for PK11195. Firstly, a Heck reaction was used to form the isoquinoline core, followed by a Suzuki reaction to couple the correct phenyl ring.