K2CO3/18-Crown-6-Catalyzed Selective H/D Exchange of Heteroarenes with Bromide as a Removable Directing Group

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Abstract

The K2CO3/18-crown-6-catalyzed H/D exchange of heretoarenes in high atom % deuterium incorporation is disclosed. The use of a weak base as a catalyst leads to excellent site selectivity and broad functional group tolerance. Control experiments indicated that the use of bromide, which enhances the adjacent C-H bond reactivity, as a removable directing group is essential. Moreover, conversion of bromide to other functional groups is also performed to construct other useful deuterated compounds.

Original languageEnglish
Pages (from-to)3055-3059
Number of pages5
JournalOrganic Letters
Volume25
Issue number17
DOIs
StatePublished - May 5 2023

Funding

This research was started when H.-H.Z. was a professor at Nanjing Tech University, and H.-H.Z. completed the manuscript while a research staff scientist at Oak Ridge National Laboratory. H.-H.Z. is currently supported by the Center for Structural Molecular Biology, sponsored by the Office of Biological and Environmental Research and supported by the Center for Nanophase Materials Sciences, which is a DOE Office of Science User Facility. We thank the National Natural Science Foundation of China (Grant 22075135).

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