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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/?mol (n = 3).

SUBMITTER: Duffy IR

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

REPOSITORIES: biostudies-literature

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

Duffy Ian R IR Vasdev Neil N Dahl Kenneth K

ACS omega 20200402 14

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- ...[more]

PMID: 32309734

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