期刊
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
卷 59, 期 1, 页码 9-13出版社
WILEY
DOI: 10.1002/jlcr.3360
关键词
[C-11]tubastatin A; HDAC6; [C-11]Carbon monoxide; Carbonylation; Hydroxyaminolysis
资金
- Intramural Research Program of the National Institutes of Health (NIMH) [ZIA-MH002793]
We aimed to label tubastatin A (1) with carbon-11 (t(1/2)=20.4min) in the hydroxamic acid site to provide a potential radiotracer for imaging histone deacetylase 6 in vivo with positron emission tomography. Initial attempts at a one-pot Pd-mediated insertion of [C-11]carbon monoxide between the aryl iodide (2) and hydroxylamine gave low radiochemical yields (<5%) of [C-11]1. Labeling was achieved in useful radiochemical yields (16.1 +/- 5.6%, n=4) through a two-step process based on Pd-mediated insertion of [C-11]carbon monoxide between the aryl iodide (2) and p-nitrophenol to give the [C-11]p-nitrophenyl ester ([C-11]5), followed by ultrasound-assisted hydroxyaminolysis of the activated ester with excess hydroxylamine in a DMSO/THF mixture in the presence of a strong phosphazene base P-1-t-Bu. However, success in labeling the hydroxamic acid group of [C-11]tubastatin A was not transferable to the labeling of three other model hydroxamic acids.
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