A concise method for fully automated radiosyntheses of [18F]JNJ-46356479 and [18F]FITM via Cu-mediated 18F-fluorination of organoboranes

Gengyang Yuan; Timothy M. Shoup; Sung-Hyun Moon; Anna-Liisa Brownell

doi:10.1039/D0RA04943C

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A concise method for fully automated radiosyntheses of [¹⁸F]JNJ-46356479 and [¹⁸F]FITM via Cu-mediated ¹⁸F-fluorination of organoboranes†

Gengyang Yuan,

*^a Timothy M. Shoup,^a Sung-Hyun Moon

^a and Anna-Liisa Brownell*^a

Author affiliations

* Corresponding authors

^a Gordon Center for Medical Imaging, Massachusetts General Hospital and Harvard Medical School, 3rd Avenue, Charlestown, MA 02129, USA
E-mail: gyyuan@mgh.harvard.edu, abrownell@mgh.harvard.edu

Abstract

A modified alcohol-enhanced ¹⁸F-fluorodeboronation has been developed for the radiosyntheses of [¹⁸F]JNJ-46356479 and [¹⁸F]FITM. Unlike the [¹⁸F]KF/K₂₂₂ approach, this method tolerates the presence of sensitive heterocycles in Bpin precursors 4 and 8 allowing a one-step ¹⁸F-fluorodeboronation on the fully automated TRACERlab™ FX_FN platform.

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Article information

DOI: https://doi.org/10.1039/D0RA04943C
Article type: Paper
Submitted: 04 Jun 2020
Accepted: 25 Jun 2020
First published: 02 Jul 2020
This article is Open Access

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RSC Adv., 2020,10, 25223-25227

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A concise method for fully automated radiosyntheses of [¹⁸F]JNJ-46356479 and [¹⁸F]FITM via Cu-mediated ¹⁸F-fluorination of organoboranes

G. Yuan, T. M. Shoup, S. Moon and A. Brownell, RSC Adv., 2020, 10, 25223 DOI: 10.1039/D0RA04943C

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. You can use material from this article in other publications without requesting further permissions from the RSC, provided that the correct acknowledgement is given.

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