Carbon‐13 labeling of ibrutinib for human microdosing
Journal of Labelled Compounds and Radiopharmaceuticals January 1, 2023 Yong Gong, Rhys Salter
A 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.