Copper(I)-Mediated ¹¹C-Carboxylation of (Hetero)arylstannanes.

ABSTRACT: A novel copper-mediated carboxylation strategy of aryl- and heteroaryl-stannanes is described. The method serves as a mild (i.e., 1 atm) carboxylation method using stable carbon dioxide and is transferable as a radiosynthetic approach for carbon-11-labeled aromatic and heteroaromatic carboxylic acids using sub-stoichiometric quantities of [¹¹C]CO₂. The methodology was applied to the radiosynthesis of the retinoid X receptor agonist, [¹¹C]bexarotene, with a decay-corrected radiochemical yield of 32 ± 5% and molar activity of 38 ± 23 GBq/μmol (n = 3).

SUBMITTER: Duffy IR 

PROVIDER: S-EPMC7161067 | biostudies-literature | 2020 Apr

REPOSITORIES: biostudies-literature