Metal oxide catalyzed radiofluorination

US9895454B2 · kind B2 · utility

Assignee

• The Regents of the University of California · US

Inventors

• Maxim Sergeev · Los Angeles, US
• Federica Morgia · Los Angeles, US
• Robert Michael Van Dam · Los Angeles, US
• Mark Lazari · San Fernando, US

Key dates

• Filing date: Jul 2, 2015
• Grant date: Feb 20, 2018
• Expiry date: Jul 2, 2035

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C2601/14
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Inter alia, the first titania-catalyzed [18F]-radiofluorination in highly aqueous medium is provided. In embodiments, the method utilizes titanium dioxide, 1:1 acetonitrile-thexyl alcohol solvent mixture and tetrabutylammonium bicarbonate as a base. Radiolabeling may be directly performed with aqueous [18F]fluoride without the need for drying/azeotroping step, which reduces radiosynthesis time while keeping high fluoride conversion. The general applicability of the synthetic strategy to the synthesis of the wide range of PET probes from tosylated precursors is demonstrated.