Carbon‐13 labeling of ibrutinib for human microdosing
Yong Gong, Rhys Salter
Journal of Labelled Compounds and Radiopharmaceuticals 2023 DOI: 10.1002/jlcr.4007 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Method development Peer reviewed |
|---|---|
| Topics | Microdosing |
| Key points | A 10-step synthesis of carbon-13 labeled ibrutinib achieved >99% chemical purity and >99% enantiomeric excess with 31% overall yield. |
Abstract
Ibrutinib is an oral medication for the treatment of B cell malignancies. During its clinical development, a stable isotopologue of ibrutinib was required for the assessment of the drug's absolute oral bioavailability via intravenous microdosing. The following work describes a 10‐step, gram‐scale production of carbon‐13 labeled ibrutinib from [13C6]phenol (13C6, 99%) in 31% overall yield with >99% chemical purity and >99% enantiomeric excess (ee), suitable for intravenous microdosing in humans.