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Site-Selective Late-Stage Aromatic [18 F]Fluorination via Aryl Sulfonium Salts.

ABSTRACT: Site-selective functionalization of C-H bonds in small complex molecules is a long-standing challenge in organic chemistry. Herein, we report a broadly applicable and site-selective aromatic C-H dibenzothiophenylation reaction. The conceptual advantage of this transformation is further demonstrated through the two-step C-H [18 F]fluorination of a series of marketed small-molecule drugs.

SUBMITTER: Xu P

PROVIDER: S-EPMC7004179 | biostudies-literature | 2020 Jan

REPOSITORIES: biostudies-literature

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Site-Selective Late-Stage Aromatic [18 F]Fluorination via Aryl Sulfonium Salts.

Xu Peng P Zhao Da D Berger Florian F Hamad Aboubakr A Rickmeier Jens J Petzold Roland R Kondratiuk Mykhailo M Bohdan Kostiantyn K Ritter Tobias T

Angewandte Chemie (International ed. in English) 20191212 5

Site-selective functionalization of C-H bonds in small complex molecules is a long-standing challenge in organic chemistry. Herein, we report a broadly applicable and site-selective aromatic C-H dibenzothiophenylation reaction. The conceptual advantage of this transformation is further demonstrated through the two-step C-H [18 F]fluorination of a series of marketed small-molecule drugs. ...[more]

PMID: 31697427

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