Production Of 11 C‐Labeled Amides Via “In‐Loop” 11 C‐Carbonylation

The carbon‐11 ( 11 C) labeling of benzamides holds great promise in the development of PET radiotracers given the prevalence of benzamides in bioactive molecules. This work establishes an improved automated route to 11 C labeled primary benzamides through carbonylative cross‐coupling of aryl halides with 11 C carbon monoxide using electrophilic aroyl dimethylaminopyridinium salts as an intermediate. The methodology uses GE TRACERLab FX automated radiochemistry synthesis modules and allows for the synthesis of a variety of benzamide containing compounds, including known PET imaging agent [ 11 C]LY2795050, a KOR antagonist, in moderate to excellent radiochemical yields. This not only provides a practical means of synthesizing primary [ 11 C]benzamides, but it sets the stage for potential future applications in PET tracer synthesis. Overall, this development offers a versatile tool for generating 11 C‐labeled compounds for PET imaging applications thus, opening new avenues in the field of molecular imaging and advancing our understanding of various biological processes.