Abstract

Positron emission tomography (PET) of labeled metabolites, drugs, proteins and nanomaterials[1-3] is rapidly emerging as a powerful imaging tool to detect and stage disease, to study human biology, to investigate pharmacokinetics and pharmacodynamics of new drugs, or to measure treatment efficacy in clinical trials.[4-8] 18F is one of the most commonly used isotopes for clinical imaging given its half-life, ease of production, wide availability, and compatibility with microfluidics syntheses.[9] Despite extensive use and well established procedures of labeling some small molecules, facile 18F platform-type universally adaptable labeling strategies are still largely missing. This is especially true for rapid labeling of small molecules that emerge from high throughput screens or for optimizing hybrid and modular imaging agents. Bioorthogonal chemistries represent one avenue to develop such generic labeling platforms.

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