期刊
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
卷 136, 期 14, 页码 5291-5294出版社
AMER CHEMICAL SOC
DOI: 10.1021/ja5025645
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资金
- Princeton University
- National Science Foundation [CAREER-1148750]
- National Institute of Health [CA164490, DK081342]
- PA Health department
- Bristol-Myers Squibb
- Eli Lilly
- National Science Foundation Graduate Research Fellowship [DGE-1148900]
- Division Of Chemistry
- Direct For Mathematical & Physical Scien [1148750] Funding Source: National Science Foundation
Herein, we describe an operationally straightforward radiosynthesis of a chiral transition metal fluoride catalyst, [F-18](salen)CoF, and its use for late-stage enantioselective aliphatic radiofluorination. We demonstrate the utility of the method by preparing single enantiomer experimental and clinically validated PET tracers that contain base-sensitive functional groups, epimerizable stereocenters, and nitrogen-rich motifs. Unlike the conventional radiosyntheses of these targets with [F-18]KF, labeling with (salen)CoF is possible in the last step and under exceptionally mild conditions. These results constitute a rare example of a nucleophilic radiofluorination using a transition metal fluoride and highlight the potential of such reagents to enhance traditional methods for labeling aliphatic hydrocarbons.
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