Duffy Ian R, Vasdev Neil, Dahl Kenneth
Azrieli Centre for Neuro-Radiochemistry, Brain Health Imaging Centre, Centre for Addiction and Mental Health, 250 College Street, Toronto, ON M5T 1R8, Canada.
Department of Psychiatry, University of Toronto, 250 College Street, Toronto, ON M5T 1R8, Canada.
ACS Omega. 2020 Apr 2;5(14):8242-8250. doi: 10.1021/acsomega.0c00524. eCollection 2020 Apr 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 [C]CO. The methodology was applied to the radiosynthesis of the retinoid X receptor agonist, [C]bexarotene, with a decay-corrected radiochemical yield of 32 ± 5% and molar activity of 38 ± 23 GBq/μmol ( = 3).
描述了一种新型的铜介导的芳基和杂芳基锡烷的羧基化策略。该方法是一种使用稳定二氧化碳的温和（即1个大气压）羧基化方法，并且可作为一种放射性合成方法，用于使用亚化学计量的[¹¹C]CO制备¹¹C标记的芳香族和杂芳香族羧酸。该方法被应用于视黄酸X受体激动剂[¹¹C]贝沙罗汀的放射性合成，经衰变校正的放射化学产率为32±5%，摩尔活度为38±23 GBq/μmol（n = 3）。
