Journal
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
Volume 136, Issue 19, Pages 6842-6845Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ja5039819
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Funding
- Center for Catalytic Hydrocarbon Functionalization, an Energy Frontier Research Center, U.S. Department of Energy, Office of Science, Basic Energy Sciences [DE SC0001298]
- US National Science Foundation [CHE-1148597]
- US Dept. of Energy radiochemistry training grant [DE-SC0008430]
- Howard Hughes Medical Institute
- Merck, Inc.
- [S10RR017208]
- [S10RR023452]
- Division Of Chemistry
- Direct For Mathematical & Physical Scien [1148597] Funding Source: National Science Foundation
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We describe the first late-stage F-18 labeling chemistry for aliphatic C-H bonds with no-carrier-added [E-18]fluoride. The method uses Mn(salen)OTs as an F-transfer catalyst and enables the facile labeling of a variety of bioactive molecules and building blocks with radiochemical yields (RCY) ranging from 20% to 72% within 10 min without the need for preactivation of the labeling precursor. Notably, the catalyst itself can directly elute [F-18]fluoride from an ion exchange cartridge with over 90% efficiency. Using this feature, the conventional and laborious dry-down step prior to reaction is circumvented, greatly simplifying the mechanics of this protocol and shortening the time for automated synthesis. Eight drug molecules, including COX, ACE, MAO, and PDE inhibitors, have been successfully [F-18]-labeled in this way.
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