- Utilizing Carbonyl Coordination of Native Amides for Palladium-Catalyzed C(sp3)?H Olefination
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PdII-catalyzed C(sp3)?H olefination of weakly coordinating native amides is reported. Three major drawbacks of previous C(sp3)?H olefination protocols, 1) in situ cyclization of products, 2) incompatibility with α-H-containing substrates, and 3) installation of exogenous directing groups, are addressed by harnessing the carbonyl coordination ability of amides to direct C(sp3)?H activation. The method enables direct C(sp3)?H functionalization of a wide range of native amide substrates, including secondary, tertiary, and cyclic amides, for the first time. The utility of this process is demonstrated by diverse transformations of the olefination products.
- Park, Hojoon,Li, Yang,Yu, Jin-Quan
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supporting information
p. 11424 - 11428
(2019/07/17)
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- Heteroaromatic sulphonamide prodrugs
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The invention relates to sulphonamide prodrugs of the general formula I, having a heteroaromatic linker, to a process for their preparation, to pharmaceutical compositions comprising these compounds and to their use for the production of orally available medicaments. The compounds according to the invention bind to carboanhydrases and inhibit these enzymes.
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Page/Page column 3
(2008/06/13)
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