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Rhodium-Catalyzed Boron Arylation of 1,2-Azaborines


  • Correspondence concerning X-ray crystallography should be directed to Lev Zakharov ( This research was supported by the National Institutes of Health (National Institute of General Medical Sciences, R01-GM094541 and R41-GM099181). Funding for the University of Oregon Chemistry Research and Instrumentation Services has been provided in part by the NSF (CHE-0923589). We thank Dr. Adam Marwitz for performing the stability assessment of BN felbinac.


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A Sn-phony in B! BN isosteres of biphenyl compounds are prepared through Rh-catalyzed cross-coupling between 2-chloro-1,2-azaborines and arylstannanes (see scheme). The synthetic method should enable investigations of structure–activity relationships (SARs) by expanding the chemical space of the pharmaceutically relevant biphenyl structure through BN/CC isosterism.

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