Metallaphotoredox aryl and alkyl radiomethylation for PET ligand discovery.

ABSTRACT: Positron emission tomography (PET) radioligands (radioactively labelled tracer compounds) are extremely useful for in vivo characterization of central nervous system drug candidates, neurodegenerative diseases and numerous oncology targets¹. Both tritium and carbon-11 radioisotopologues are generally necessary for in vitro and in vivo characterization of radioligands², yet there exist few radiolabelling protocols for the synthesis of either, inhibiting the development of PET radioligands. The synthesis of such radioligands also needs to be very rapid owing to the short half-life of carbon-11. Here we report a versatile and rapid metallaphotoredox-catalysed method for late-stage installation of both tritium and carbon-11 into the desired compounds via methylation of ph

SUBMITTER: Pipal RW 

PROVIDER: S-EPMC7856055 | biostudies-literature | 2021 Jan

REPOSITORIES: biostudies-literature