Carbon‐13 labeling of ibrutinib for human microdosing
Journal of Labelled Compounds and Radiopharmaceuticals January 1, 2023 DOI: 10.1002/jlcr.4007 (opens in new tab)
Summary
AI-generated from the abstractA 10-step, gram-scale method produced carbon-13 labeled ibrutinib from [13C6]phenol with 31% overall yield, >99% chemical purity, and >99% enantiomeric excess, suitable for intravenous microdosing in humans to assess the drug's absolute oral bioavailability.
Study at a glance
| Characteristics | Method development Peer reviewed |
|---|---|
| Key finding | 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.