Journal
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
Volume 134, Issue 29, Pages 12239-12244Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ja3041338
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Funding
- Sanofi-Aventis Deutschland GmbH
- BMBF (Bundesministerium fur Bildung and Forschung)
- Deutsche Forschungsgemeinschaft [DFG BE 1931/16-1]
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A novel and convenient protocol for the catalytic hydrogen-deuterium exchange of biologically active tertiary amines utilizing the borrowing hydrogen methodology has been developed. In the presence of the readily available Shvo catalyst, excellent chemoselectivity toward alpha- and beta-protons with respect to the nitrogen atom as well as high degree of deuterium incorporation and functional group tolerance is achieved. This allowed for the deuteration of complex pharmaceutically interesting substrates, including examples for actual marketed drug compounds. Notably, this method constitutes a powerful tool for the generation of valuable internal standard materials for LC-MS/MS analyses highly demanded for various life-science applications.
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