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

doi:10.1016/j.tetlet.2015.01.074

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

Tetrahedron Lett. 2015 Jun 3;56(23):3620-3623. doi: 10.1016/j.tetlet.2015.01.074.

Authors

T Aaron Bedell^#¹, Graham A B Hone^#¹, Justin Du Bois², Erik J Sorensen¹

Affiliations

¹ Department of Chemistry, Princeton University, Princeton, NJ 08544, United States.
² Department of Chemistry, Stanford University, Stanford, California 94305, United States.

^# Contributed equally.

Abstract

A new, concise synthesis of the CCR-5 receptor antagonist maraviroc (UK-427,857) from 3-phenyl-1-propanol has been completed in four steps featuring a site-selective C-H functionalization.

Keywords: Amination; C-H functionalization; CCR-5; HIV/AIDS; Maraviroc.

Grants and funding

R01 GM065483/GM/NIGMS NIH HHS/United States