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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.


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™ FXFN platform.

SUBMITTER: Yuan G 

PROVIDER: S-EPMC7497470 | biostudies-literature | 2020 Jul

REPOSITORIES: biostudies-literature

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A concise method for fully automated radiosyntheses of [<sup>18</sup>F]JNJ-46356479 and [<sup>18</sup>F]FITM <i>via</i> Cu-mediated <sup>18</sup>F-fluorination of organoboranes.

Yuan Gengyang G   Shoup Timothy M TM   Moon Sung-Hyun SH   Brownell Anna-Liisa AL  

RSC advances 20200701 42


A modified alcohol-enhanced <sup>18</sup>F-fluorodeboronation has been developed for the radiosyntheses of [<sup>18</sup>F]JNJ-46356479 and [<sup>18</sup>F]FITM. Unlike the [<sup>18</sup>F]KF/K<sub>222</sub> approach, this method tolerates the presence of sensitive heterocycles in Bpin precursors <b>4</b> and <b>8</b> allowing a one-step <sup>18</sup>F-fluorodeboronation on the fully automated TRACERlab™ FX<sub>FN</sub> platform. ...[more]

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