Synthesis of 2,3-Disubstituted 4‑Ethoxycarbonyl-β-carbolin-1-ones: Application to the Synthesis of SL651498 and Its Analogue

Synthesis of 2,3-disubstituted 4-ethoxycarbonyl-β-carbolin-1-ones is developed using palladium-catalyzed intramolecular amination of 3-amino-4-(2-bromophenyl)-2-pyridones prepared by the conjugate addition reaction of diethyl 2-aminomalonate to alkynyl imines. The method was applied to the total syn...

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Published inACS omega Vol. 5; no. 25; pp. 15631 - 15656
Main Authors Miura, Ryoya, Goto, Shinsuke, Hashimoto, Takahide, Hachiya, Iwao
Format Journal Article
LanguageEnglish
Published American Chemical Society 30.06.2020
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Summary:Synthesis of 2,3-disubstituted 4-ethoxycarbonyl-β-carbolin-1-ones is developed using palladium-catalyzed intramolecular amination of 3-amino-4-(2-bromophenyl)-2-pyridones prepared by the conjugate addition reaction of diethyl 2-aminomalonate to alkynyl imines. The method was applied to the total syntheses of SL651498 exhibiting anxiolytic activity and its analogue.
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ISSN:2470-1343
2470-1343
DOI:10.1021/acsomega.0c01854