Office of Technology Transfer – University of Michigan

Generation of Ag18F and its use in the synthesis of PET radiotracers

Technology #6465

UM File # 6465

Background

Technology Description

Applications
Advantagesission tomography (PET) is an imaging technique that relies on the decay of radioactive elements within a small molecule probe to produce an image of the spatial distribution of the probe in diseased tissues. Despite its promising applications in fields like oncology, neurology, and cardiology; PET has seen limited adaptation in this fields due to a lack of methodology for synthesizing potent radiotracers. 18F is one of the most promising radioactive elements for PET, however its incorporation into the organic rings that make up many biological molecules presents an enormous challenge to organic chemists who have thus far struggled to produce radiochemical yields that are sufficient for clinical applications. We have developed new technologies for production of nucleophillic 18F sources that make fluorine radiochemistry increasingly accessible to chemists who need to synthesize radiotracers on demand and on location for clinical purposes. These methods offer new synthetic routes to attractive targets for PET radiotracers.

Rapid Preparation of Ag18F is Crucial for Clinical Applications

Due to the relatively short half-life of 18F, rapid enrichment and synthetic procedures must be used in order to produce a potent radiopharmaceutical for clinical diagnostics. We have identified a facile method for elution of Ag18F from Sep-Pak columns prior to use as a nucleophillic fluorine source in the copper mediated fluorination of aryl iodides. Aryl iodides are the gold standard radiopharmaceutical precursors due to their exceptional shelf life and the ease and specificity with which they react with nucleophillic fluorine sources. This technology allows for fast preparation of Ag18F as well as rapid and mild synthesis of final radiohpharmaceutical products from stock iodide precursors. Due to the diversity of biologically relevant iodide precursors that can be readily synthesized, this technology will create tremendous diversity in the structural space compatible with 18F for radiopharmaceutical applications.

Applications

  • Facile synthesis of Ag18F for efficient synthesis of radiopharmaceuticals
  • Novel late-stage fluorination reactions for development of new radiopharmaceuticals

Advantages

  • Utilizes soluble silver sources and widely available, inexpensive equipment
  • Allows for late stage fluorination of radiopharmaceutical precursors on demand and on location
  • Accesses new chemical space for 18F radiopharmaceuticals