Journal
CHEMICAL SCIENCE
Volume 13, Issue 40, Pages 11878-11882Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/d2sc04605a
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Funding
- National Institute of General Medical Sciences [R35 GM131708]
- National Science Foundation
- [CHE-1726291]
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The late-stage introduction of diverse heterocycles onto complex small molecules enables efficient access to new medicinally relevant compounds. Here, we report a system that enables direct C-H heteroarylation using a stable, commercially available O-alkenylhydroxamate with heterocyclic sulfone partners. The C-H heteroarylation proceeds efficiently with a range of aliphatic substrates and common heterocycles, and is a rare example of heteroarylation of strong C-H bonds. Importantly, the present approach is amenable to late-stage functionalization as the substrate is the limiting reagent in all cases.
The late-stage introduction of diverse heterocycles onto complex small molecules enables efficient access to new medicinally relevant compounds. An attractive approach to such a transformation would utilize the ubiquitous aliphatic C-H bonds of a complex substrate. Herein, we report a system that enables direct C-H heteroarylation using a stable, commercially available O-alkenylhydroxamate with heterocyclic sulfone partners. The C-H heteroarylation proceeds efficiently with a range of aliphatic substrates and common heterocycles, and is a rare example of heteroarylation of strong C-H bonds. Importantly, the present approach is amenable to late-stage functionalization as the substrate is the limiting reagent in all cases.
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