Convenient and straightforward synthesis of ibrutinib labeled by carbon-13 isotope is reported. Isotopically labeled building block is introduced in the last step of reaction sequence affording sufficient isolated yield (7%) of [13 C6 ]-ibrutinib calculated towards starting commercially available [13 C6 ]-bromobenzene.

Faculty of Medicine in Hradec Kralove Charles University Hradec Kralove Czech Republic

Institute of Organic Chemistry and Biochemistry The Czech Academy of Sciences Prague Czech Republic

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