Organosilicon Precursors for Efficient Aromatic Copper-Mediated Radiocyanation.

ABSTRACT: Copper-mediated radiolabelling has transformed how (hetero)aromatic imaging agents are prepared for positron emission tomography (PET). However, current methods maintain critical stability, reactivity, and toxicity concerns paramount for safely and reproducibly generating radiomedicines. To overcome these limitations, a copper-mediated ¹¹C-cyanation reaction is presented that leverages heptamethyltrisiloxanes as (hetero)aryl nucleophiles. Rapid ipso-radiocyanation occurs in conversions surpassing related precursors, while offering stability and safety advantages. Multiple bioactive scaffolds relevant to (pre)clinical PET were labelled to showcase the broader significance of this protocol. Most notably, an automated radiosynthesis of a κ-opioid receptor antagonist currentl

SUBMITTER: Wright JS 

PROVIDER: S-EPMC12419773 | biostudies-literature | 2025 Aug

REPOSITORIES: biostudies-literature