ChemRxiv
These are preliminary reports that have not been peer-reviewed. They should not be regarded as conclusive, guide clinical practice/health-related behavior, or be reported in news media as established information. For more information, please see our FAQs.
furopyridine chemrxiv final.pdf (1.47 MB)
0/0

Concise, Gram-Scale Synthesis of Furo[2,3-B]pyridines, with Functional Handles for Chemoselective Cross-Coupling

preprint
submitted on 16.03.2020 and posted on 17.03.2020 by Sean O'Byrne, Benjamin J. Eduful, Timothy M. Willson, David Drewry

A concise 4-step synthesis of furo[2,3-b]pyridines, with handles in the 3 and 5 positions for palladium mediated cross-coupling reactions, is described. The synthetic route has been optimized, with only one step requiring purification by column chromatography. The route is amenable to scaling-up and was successfully executed on a multi-gram scale. Furopyridines are of growing interest in medicinal chemistry, and this route should enable easy access to the core for structure-activity relationship (SAR) studies.

Funding

Creation of in vivo active chemical probes for CAMKK2 to treat cancer

National Cancer Institute

Find out more...

1U24DK116204-01

History

Email Address of Submitting Author

david.drewry@unc.edu

Institution

UNC Eshelman School of Pharmacy

Country

United States

ORCID For Submitting Author

0000-0001-5973-5798

Declaration of Conflict of Interest

no conflict of interest

Exports