Washington University

Dong Zhou

Wenhua Chu

Robert H Mach

Loren Michel

Delphine Chen

Described herein are methods and devices that allow the generation of [F-18]triflyl fluoride and other [F-18] sulfonyl fluorides (such as [F-18]tosyl fluoride) in a manner that is suitable for radiosynthesis of F-18 labeled radiopharmaceuticals using currently available synthesis modules.

Methods and devices to generate [F-18]triflyl fluoride and other [F-18] sulfonyl fluorides

The present disclosure relates to the methods for the preparation of reactive [F-18]fluoride in a form of [F-18]sulfonyl fluoride suitable for efficient radiolabeling without an azeotropic evaporation step by the use of anion exchange resin and sulfonyl chloride, and its applications in the manufacturing of PET radiopharmaceuticals.

Synthesizing pet tracers using [F-18]sulfonyl fluoride as a source of [F-18]fluoride

Disclosed are PARP-1 inhibitors, which can beF-labeled for use as tracers in positron emission tomographic (PET) imaging. Further disclosed are methods of synthesis. Of the compounds synthesized, 2-[p-(2-Fluoroethoxy)phenyl]-1.3.10-triazatricyclo[6.4.1.0]trideca-2,4(13),5,7-tetraen-9-one (12) had the highest inhibition potency for PARP-1 (IC=6.3 nM). Synthesis of [F]-12 is disclosed under conventional conditions in high specific activity with 40-50% decay-corrected yield. MicroPET imaging using [F]-12 in MDA-MB-436 tumor-bearing mice demonstrated accumulation of [F]-12 in a tumor. Binding, can be blocked by olaparib. The compounds have utility for tumor imaging.

Growing community of inventors

St. Louis, MO, United States of America

Dong Zhou