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

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

RSC Adv. 2020 Jul 2;10(42):25223-25227. doi: 10.1039/d0ra04943c.

Authors

Gengyang Yuan¹, Timothy M Shoup¹, Sung-Hyun Moon¹, Anna-Liisa Brownell¹

Affiliation

¹ Gordon Center for Medical Imaging, Massachusetts General Hospital and Harvard Medical School, 3rd Avenue, Charlestown, MA 02129, USA. Email: [email protected]; Email: [email protected].

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.

Abstract

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