Automated production of 11C ‐labeled carboxylic acids and esters via “in‐loop” 11C‐carbonylation using GE FX synthesis modules

An in-loop11C-carbonylation process for the radiosynthesis of11C-carboxylic acids and esters from halide precursors is reported. The reaction proceeds at room temperature and enables11C-carbonylation of both electron deficient and electron rich (hetero)aromatic halides to provide11C-carboxylic acids and esters in good to excellent radiochemical yields, high radiochemical purity, and excellent molar activity. The process has been fully automated using commercial radiochemistry synthesis modules, and suitability for clinical production is demonstrated via validated radiosyntheses of [11C]bexarotene and [11C]acetoacetic acid. An in-loop11C-carbonylation process for the radiosynthesis of11C-carboxylic acids and esters from halide precursors has been developed. The reaction proceeds at room temperature under mild conditions and enables11C-carbonylation of both electron deficient and electron rich (hetero)aromatic halides to provide11C-carboxylic acids and esters in good to excellent radiochemical yields, high radiochemical purity, and excellent molar activity. The process has been fully automated using commercial radiochemistry synthesis modules, and application to clinical production is demonstrated via validated cGMP radiosyntheses of [11C]bexarotene and [11C]acetoacetic acid.

Source: Journal of Labelled Compounds and Radiopharmaceuticals - August 23, 2023 Category: Biochemistry Authors: Tanpreet Kaur, Jay S. Wright, Bradford D. Henderson, Jonathan Godinez, Xia Shao, Peter J. H. Scott Tags: RESEARCH ARTICLE Source Type: research