Straightforward synthesis of PET tracer precursors used for the early diagnosis of Alzheimers disease through Suzuki–Miyaura cross-coupling reactions

In positron emission tomography [11C]PIB, Pittsburgh Compound-B, is currently the most widely used radiopharmaceutical for the early diagnosis of Alzheimerʹs disease. Synthetic routes for the preparation of the precursor of [11C]PIB are reported in the literature. These strategies require multiple steps and the use of protecting groups. This paper describes a simple one-step synthesis of the precursor of [11C]PIB through a Suzuki–Miyaura coupling reaction using thermal conditions or microwave activation. These methods were successfully applied to the synthesis of various 2-arylbenzothiazole and 2-pyridinylbenzothiazole compounds including [18F] precursor derivatives of PIB containing a nitro function.