Synthesis of [13C6]-ibrutinib

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 [C-13(6)]-ibrutinib calculated towards starting commercially available [C-13(6)]-bromobenzene.

Automated summary

A convenient and straightforward method for synthesizing ibrutinib labeled with carbon-13 isotope was reported, achieving a sufficient isolated yield of [C-13(6)]-ibrutinib in the final step of the reaction sequence. The yield was calculated based on commercially available [C-13(6)]-bromobenzene.