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Novel 18F-Fluorinated Amino Acids as Oncological PET Radiotracers

New process for creating radiolabeled compounds with short radiosynthesis time without racemization of starting material or products

Background

Radiolabeled amino acids have been used for PET imaging of tumors for decades. Of the naturally occurring amino acids, leucine is particularly important to cancer biology and shows significant uptake in many types of primary and metastatic tumor sites. However, traditional strategies for incorporating radionuclides into leucine require difficult-to-synthesize precursors and chemically harsh conditions (high temperatures, harsh reagents) that are incompatible with radiotracer production. Hence, there is a real need for simple and robust synthesis processes for the preparation of radiolabeled amino acids, and particularly derivatives of leucine, that can be used for detection and treatment monitoring of cancer.

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