Carbon ‐13 labeling of ibrutinib for human microdosing

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 ten-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.
Source: Journal of Labelled Compounds and Radiopharmaceuticals - Category: Biochemistry Authors: Tags: PRACTITIONER PROTOCOL ‐ SYNTHESIS Source Type: research