Synthesis of imatinib, a tyrosine kinase inhibitor, labeled with carbon ‐14

In this study, we report the synthetic optimization for14C ‐labeling and radiosynthesis of [14C]imatinib to analyze binding with cellular proteins using accelerator mass spectroscopy (AMS).14C ‐labeling of imatinib was performed by the synthesis of14C ‐labeld 2‐aminopyrimidine intermediate using [14C]guanidine ·HCl, which includes anin ‐situ reduction of an inseparable byproduct for easy purification by HPLC, followed by a cross ‐coupling reaction with aryl bromide precursor. The radiosynthesis of [14C]imatinib (specific activity, 631 MBq/mmol; radiochemical purity, 99.6%) was achieved in six steps with a total chemical yield of 29.2%.
Source: Journal of Labelled Compounds and Radiopharmaceuticals - Category: Biochemistry Authors: Tags: RESEARCH ARTICLE Source Type: research