期刊
ORGANIC PROCESS RESEARCH & DEVELOPMENT
卷 12, 期 4, 页码 637-645出版社
AMER CHEMICAL SOC
DOI: 10.1021/op600280g
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AG13736 (Axitinib), an inhibitor of vascular endothelial growth factor (VEGF) under investigation as an oncology drug, is currently manufactured via a three-step process that utilizes two palladium-mediated cross-couplings. Historically, removal of residual heavy metals from the active pharmaceutical ingredient has been a persistent issue. The development of a much improved process for palladium removal and a useful screening technique developed to rapidly identify the most efficient reagents for this purpose are outlined. The performance of the new endgame process in pilot-plant scale-up is also discussed.
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