Radiosynthesis of the D2/3 agonist [3-11C]-(+)-PHNO using [11C]iodomethane

Garcia-Arguello, Segundo Francisco; Fortt, Robin; Steel, Colin; Bričkutė, Diana; Glaser, Matthias; Turton, David R.; Robins, Edward G.; Årstad, Erik; Luthra, Sajinder K.

doi:10.1016/j.apradiso.2012.11.009

Cited by 6 publications

(1 citation statement)

References 10 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…59,60 However, the synthetic apparatus needed for multi-step reactions using Grignard reagent precursors are challenging to maintain and operate, often leading to high failure rates of radiosynthesis (see, for example, the remarkable preparation of [ 11 C]lapatinib 61 ), and generate an strong impetus to develop alternative methods that are simpler to operate and provide greater reliability. 62,63 …”

Section: [11c]co2-fixationmentioning

confidence: 99%

¹¹CO bonds made easily for positron emission tomography radiopharmaceuticals

et al. 2016

View full text Add to dashboard Cite

The positron-emitting radionuclide carbon-11 (11C, t1/2 = 20.3 minutes) possesses the unique potential for radiolabeling of any biological, naturally occurring, or synthetic organic molecule for in vivo positron emission tomography (PET) imaging. Carbon-11 is most often incorporated into small molecules by methylation of alcohol, thiol, amine or carboxylic acid precursors using [11C]methyl iodide or [11C]methyl triflate (generated from [11C]CO2). Consequently, small molecules that lack an easily substituted 11C-methyl group are often considered to have non-obvious strategies for radiolabeling and require a more customized approach. [11C]Carbon dioxide, [11C]carbon monoxide, [11C]cyanide, and [11C]phosgene represent alternative carbon-11 reactants to enable 11C-carbonylation. Methodologies developed for preparation of 11C-carbonyl groups have had a tremendous impact on the development of novel PET radiopharmaceuticals and provided key tools for clinical research. 11C-Carbonyl radiopharmaceuticals based on labeled carboxylic acids, amides, carbamates, and ureas now account for a substantial number of important imaging agents that have seen translation to higher species and clinical research of previously inaccessible targets, which is a testament to the creativity, utility, and practicality of the underlying radiochemistry.

show abstract