3 years ago
Development of a sp2–sp3 Stille Cross-Coupling for Rapid Synthesis of HIV NNRTI Doravirine Analogues
Antonella Converso, Mark Campbell, Abdellatif ElMarrouni, James J. Perkins
The development of a C(sp2)–C(sp3) cross-coupling reaction for rapid, parallel synthesis of analogues of two HIV NNRTI clinical candidates is described. This method allowed easy access to the C-ring space using a practical alkylation with commercially available tributyl(iodomethyl)stannane followed by a palladium-catalyzed coupling with a variety of aryl halides (I, Br) in the presence of copper chloride. Optimization and scope of this method are reported.
Publisher URL: http://dx.doi.org/10.1021/acs.orglett.7b01142
DOI: 10.1021/acs.orglett.7b01142
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