Synthesis of Kappa Opioid Antagonists Based On Pyrrolo[1,2-α]quinoxalinones Using an N-Arylation/Condensation/Oxidation Reaction Sequence.
Synthesis of Kappa Opioid Antagonists Based On Pyrrolo[1,2-α]quinoxalinones Using an N-Arylation/Condensation/Oxidation Reaction Sequence.
复制标题
使用 N-芳基化/缩合/氧化反应序列合成基于吡咯并[1,2-α]喹喔啉酮的 Kappa 阿片拮抗剂。
DOI：
10.1021/acs.joc.6b01350
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发表时间：
2016
期刊：
影响因子：
--
通讯作者：
Aubé,Jeffrey
中科院分区：
文献类型：
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作者：
Scarry,SarahM;Lovell,KimberlyM;Frankowski,KevinJ;Bohn,LauraM;Aubé,Jeffrey
氮杂环的喹诺啉和喹诺啉酮家族存在于从感染性疾病到神经科学靶点的各种治疗相关分子中。在这里，我们描述了从市售原料中合成吡咯[1,2-α]喹诺沙林酮的一般合成序列及其在制备潜在的kappa阿片受体拮抗剂中的应用。本文简要介绍并讨论了从后一组化合物中获得的生物学数据。
The quinoxaline and quinoxalinone family of nitrogen heterocycles is present in molecules of therapeutic relevance for diverse applications ranging from infectious diseases to neuroscience targets. Here, we describe a general synthetic sequence to afford pyrrolo[1,2-α]quinoxalinones from commercially available starting materials and their use in preparing potential kappa opioid receptor antagonists. The biological data obtained from the latter set of compounds is briefly presented and discussed.