Late-Stage 18 F-Difluoromethyl Labeling of N-Heteroaromatics with High Molar Activity for PET Imaging.
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ABSTRACT:
SUBMITTER: Trump L
PROVIDER: S-EPMC6790700 | biostudies-literature | 2019 Sep
REPOSITORIES: biostudies-literature
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Late-Stage <sup>18</sup> F-Difluoromethyl Labeling of N-Heteroaromatics with High Molar Activity for PET Imaging.
Trump Laura L Lemos Agostinho A Lallemand Bénédicte B Pasau Patrick P Mercier Joël J Lemaire Christian C Luxen André A Genicot Christophe C
Angewandte Chemie (International ed. in English) 20190809 37
Despite a growing interest in CHF<sub>2</sub> in medicinal chemistry, there is a lack of efficient methods for the insertion of CHF<sup>18</sup> F into druglike compounds. Herein described is a photoredox flow reaction for <sup>18</sup> F-difluoromethylation of N-heteroaromatics that are widely used in medicinal chemistry. Following the two-step synthesis for a new <sup>18</sup> F-difluoromethylation reagent, the photoredox reaction is completed within two minutes and proceeds by C-H activation, ...[more]
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