4.8 Article

An Organometallic Gold(III) Reagent for 18F Labeling of Unprotected Peptides and Sugars in Aqueous Media

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ORGANIC LETTERS
卷 24, 期 28, 页码 5132-5136

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AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.2c01965

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  1. American Cancer Society [132467-RSG-18-149-01-CCE]
  2. National Institute of General Medical Sciences [R35GM124746]

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This study reports a method for labeling unprotected peptides and sugars with a Au(III)-[F-18]fluoroaryl complex, which can generate F-18-labeled S-aryl bioconjugates in an aqueous environment in 15 minutes with high yields and excellent functional group tolerance. The method utilizes a stable organometallic Au(III) complex and highlights the versatility of designer organometallic reagents as efficient agents for rapid radiolabeling.
The 18F labeling of unprotected peptides and sugars with a Au(III)-[F-18]fluoroaryl complex is reported. The chemoselective method generates F-18-labeled S-aryl bioconjugates in an aqueous environment in 15 min with high radiochemical yields and displays excellent functional group tolerance. This approach utilizes an air and moisture stable, robust organometallic Au(III) complex and highlights the versatility of designer organometallic reagents as efficient agents for rapid radiolabeling.

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