An expedient synthesis of maraviroc (UK-427,857) via C–H functionalization

T. Aaron Bedell, Graham A.B. Hone, Justin Du Bois, Erik J. Sorensen

Tetrahedron Letters,
2015, 56, 23, 3620-3623; 10.1016/j.tetlet.2015.01.074


A collaborative project between the Sorensen and Du Bois groups have employed C–H amination to streamline the synthesis of maraviroc, a frontline medication for the treatment of HIV developed by Pfizer.

The chemistry developed by the Du Bois group was found to be extremely efficient for the installation of the nitrogen containing benzylic stereocenter. The Sorensen group optimized the transformation and demonstrated its application in the synthesis of this powerful therapeutic agent.

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