Journal
ORGANIC LETTERS
Volume 20, Issue 7, Pages 1752-1755Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.8b00232
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Funding
- Department of Energy [DE-SC0017250646]
- [5T32DA028874-07]
- NATIONAL INSTITUTE ON DRUG ABUSE [T32DA028874] Funding Source: NIH RePORTER
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Access to At-211- and I-125-radiolabeled compounds in excellent RCCs and RCYs was achieved in just 10 min at room temperature using a Cu catalyst. The reaction conditions are applicable to a broad class of aryl and heteroaryl boronic reagents with varying steric and electronic properties as well as late-stage astatination and iodination of anticancer PARP inhibitors. This protocol eliminates the traditional need for toxic organotin reagents, elevated temperatures, and extended reaction times, providing a more practical and environmentally friendly approach to developing a-emitting radiotherapeutics.
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