2,3-二取代-4-乙氧羰基-β-咔啉-1-酮的合成：应用于SL651498及其类似物的合成
Synthesis of 2,3-Disubstituted 4-Ethoxycarbonyl-β-carbolin-1-ones: Application to the Synthesis of SL651498 and Its Analogue.
作者信息
Miura Ryoya, Goto Shinsuke, Hashimoto Takahide, Hachiya Iwao
机构信息
Department of Chemistry for Materials, Graduate School of Engineering, Mie University, Tsu Mie 514-8507, Japan.
出版信息
ACS Omega. 2020 Jun 16;5(25):15631-15656. doi: 10.1021/acsomega.0c01854. eCollection 2020 Jun 30.
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.
利用钯催化的分子内胺化反应，以丙二酸二乙酯与炔基亚胺的共轭加成反应制备的3-氨基-4-(2-溴苯基)-2-吡啶酮为原料，开发了2,3-二取代-4-乙氧羰基-β-咔啉-1-酮的合成方法。该方法应用于具有抗焦虑活性的SL651498及其类似物的全合成。
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