Anacetrapib
A new palladium-catalysed C-H fluorination reaction offers a concise late-stage route to anacetrapib (Chem Commun 2021)
Original title: Pd-Catalysed direct C(sp2)-H fluorination of aromatic ketones: concise access to anacetrapib
This paper reports the first palladium-catalysed direct ortho C(sp2)-H fluorination of aromatic ketones, a reaction with good regioselectivity and simple operation that provides an alternative shortcut for accessing fluorinated ketones. Using this late-stage C-H fluorination as the key step, the authors achieved a concise chemical synthesis of anacetrapib, demonstrating the new fluorination method's practical utility for building complex fluorinated drug molecules.
Original abstract
The Pd-cataylsed direct ortho-C(sp2)-H fluorination of aromatic ketones has been developed for the first time. The reaction features good regioselectivity and simple operations, constituting an alternative shortcut to access fluorinated ketones. A concise synthesis of anacetrapib has also been achieved by using late-stage C-H fluorination as a key step.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 18 August 2026. Methods.