A Radiolabeled Synthesis of Indole-C-14 LY317615, a PKC Inhibitor

摘要

We have recently developed a radiolabeled synthesis of [indole-C-14]-LY317615, a Protein Kinase C inhibitor currently in clinical trial. We desired the radiolabel to be in a metabolically robust position and chose the N-methylindole portion of the molecule. Our route involves the preparation of C-14 radiolabeled indole in the two position utilizing the Fukuyama indole synthesis and coupling with the "Eastern" piece to complete the synthesis.