3 years ago

Development of a sp2–sp3 Stille Cross-Coupling for Rapid Synthesis of HIV NNRTI Doravirine Analogues

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

You might also like
Never Miss Important Research

Researcher is an app designed by academics, for academics. Create a personalised feed in two minutes.
Choose from over 15,000 academics journals covering ten research areas then let Researcher deliver you papers tailored to your interests each day.

  • Download from Google Play
  • Download from App Store
  • Download from AppInChina

Researcher displays publicly available abstracts and doesn’t host any full article content. If the content is open access, we will direct clicks from the abstracts to the publisher website and display the PDF copy on our platform. Clicks to view the full text will be directed to the publisher website, where only users with subscriptions or access through their institution are able to view the full article.