Manufacturing 6-[18F]Fluoro- L-DOPA via Flow Chemistry-Enhanced Photoredox Radiofluorination

Xuedan Wu; Wei Chen; Huaifu Deng; Li Wang; David A Nicewicz; Zibo Li; Zhanhong Wu

doi:10.1021/acs.orglett.4c01114

Manufacturing 6-[¹⁸F]Fluoro- L-DOPA via Flow Chemistry-Enhanced Photoredox Radiofluorination

Org Lett. 2024 May 10. doi: 10.1021/acs.orglett.4c01114. Online ahead of print.

Authors

Xuedan Wu^{1

2}, Wei Chen¹, Huaifu Deng¹, Li Wang¹, David A Nicewicz³, Zibo Li¹, Zhanhong Wu¹

Affiliations

¹ Biomedical Research Imaging Center, Department of Radiology, and UNC Lineberger Comprehensive Cancer Center, University of North Carolina-Chapel Hill, 125 Mason Farm Road, Marsico Hall, Chapel Hill, North Carolina 27599, United States.
² LED Radiofluidics Corp., 250 Bell Tower Drive, Genome Science Building, Chapel Hill, North Carolina 27599, United States.
³ Department of Chemistry, University of North Carolina-Chapel Hill, 125 South Road, Chapel Hill, North Carolina 27514, United States.

PMID: 38728659
DOI: 10.1021/acs.orglett.4c01114

Abstract

In this study, we introduce a practical methodology for the synthesis of PET probes by seamlessly combining flow chemistry with photoredox radiofluorination. The clinical PET tracer 6-[¹⁸F]FDOPA was smoothly prepared in a 24.3% non-decay-corrected yield with over 99.0% radiochemical purity (RCP) and enantiomeric excess (ee), notably by a simple cartridge-based purification. The flow chemistry-enhanced photolabeling method supplies an efficient and versatile solution for the synthesis of 6-[¹⁸F]FDOPA and for more PET tracer development.