Synthesis of [13 C6 ]-ibrutinib

J Labelled Comp Radiopharm. 2021 Nov;64(13):500-512. doi: 10.1002/jlcr.3944. Epub 2021 Sep 20.

Abstract

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.

Keywords: [13C6]-ibrutinib; carbon-13; cost-effective synthesis; stable isotope labeling.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenine / analogs & derivatives*
  • Adenine / chemistry
  • Bromobenzenes / chemistry
  • Carbon Isotopes / chemistry
  • Chemistry Techniques, Synthetic / methods
  • Piperidines / chemistry*
  • Protein Kinase Inhibitors / chemistry*

Substances

  • Bromobenzenes
  • Carbon Isotopes
  • Piperidines
  • Protein Kinase Inhibitors
  • ibrutinib
  • bromobenzene
  • Adenine