Electrooxidative Metal‐Free Dehydrogenative α‐Sulfonylation of 1H‐Indole with Sodium Sulfinates
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DOI: 10.1002/ejoc.201700269
Abstract: A method for the electrochemical α-sulfonylation of 1H-indole with arenesulfinates was developed. A variety of indoles underwent this sulfonylation smoothly at room temperature under metal-free and chemical-oxidant-free conditions to afford indolyl aryl sulfones in good… read more here.
Keywords: electrooxidative metal; sulfonylation; dehydrogenative sulfonylation; sulfonylation indole ... See more keywords
Mechanistic Modeling of Lys745 Sulfonylation in EGFR C797S Reveals Chemical Determinants for Inhibitor Activity and Discriminates Reversible from Irreversible Agents
Sign Up to like & getrecommendations! Published in 2023 at "Journal of Chemical Information and Modeling"
DOI: 10.1021/acs.jcim.2c01586
Abstract: Targeted covalent inhibitors hold promise for drug discovery, particularly for kinases. Targeting the catalytic lysine of epidermal growth factor receptor (EGFR) has attracted attention as a new strategy to overcome resistance due to the emergence… read more here.
Keywords: sulfonylation; activity; mechanics; egfr ... See more keywords
Visible-Light-Mediated Late-Stage Sulfonylation of Anilines with Sulfonamides.
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DOI: 10.1021/acs.orglett.1c04144
Abstract: A visible-light-mediated late-stage sulfonylation of anilines with sulfonamides under simple reaction conditions is presented. Various primary or secondary sulfonamides including several pharmaceuticals were incorporated successfully via N-S bond activation and C-H bond sulfonylation. The synthetic… read more here.
Keywords: sulfonylation; mediated late; late stage; visible light ... See more keywords
Electrochemical C-H Sulfonylation of Hydrazones.
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DOI: 10.1021/acs.orglett.3c00999
Abstract: We have developed an electrochemical method for the direct C-H sulfonylation of aldehyde hydrazones using sodium sufinates as the sulfonylating agent under supporting electrolyte-free conditions. This straightforward sulfonylation strategy afforded a library of (E)-sufonylated hydrazones… read more here.
Keywords: electrochemical sulfonylation; sulfonylation; sulfonylation hydrazones;
Visible-Light-Promoted Selective Sulfonylation and Selenylation of Dienes to Access Sulfonyl-/Seleno-benzazepine Derivatives.
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DOI: 10.1021/acs.orglett.3c01550
Abstract: A novel visible-light-promoted selective sulfonylation and selenylation of dienes with selenosulfonates has been developed. This technology provides mild access to a wide range of sulfonyl benzo[b]azepinones and seleno-benzo[b]azepines. Preliminary mechanistic studies suggest that the sulfonylation… read more here.
Keywords: sulfonylation; light promoted; selenylation; selective sulfonylation ... See more keywords
Electrosynthesis of functionalized tetrahydrocarbazoles via sulfonylation triggered cyclization reaction of indole derivatives
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DOI: 10.1039/d1gc00609f
Abstract: Synthesis of tetrahydrocarbazoles is of great interest due to its importance in organic and biological chemistry. A method for access to such heterocyclic compounds usually needs harsh reaction conditions or transition-metal catalysts. Herein, we developed… read more here.
Keywords: indole derivatives; functionalized tetrahydrocarbazoles; electrosynthesis functionalized; reaction ... See more keywords