基于吡咯并[1,2-α]喹喔啉酮的κ阿片受体拮抗剂的合成：采用 N-芳基化/缩合/氧化反应序列。
Synthesis of Kappa Opioid Antagonists Based On Pyrrolo[1,2-α]quinoxalinones Using an N-Arylation/Condensation/Oxidation Reaction Sequence.
机构信息
Division of Chemical Biology and Medicinal Chemistry, University of North Carolina , 125 Mason Farm Road, CB 7363, Chapel Hill, North Carolina 27599, United States.
Departments of Molecular Therapeutics and Neuroscience, The Scripps Research Institute , 130 Scripps Way, #2A2, Jupiter, Florida 33458, United States.
出版信息
J Org Chem. 2016 Nov 4;81(21):10538-10550. doi: 10.1021/acs.joc.6b01350. Epub 2016 Aug 2.
Abstract
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.
摘要
喹喔啉和喹喔啉酮类氮杂环存在于具有治疗相关性的分子中，这些分子的应用范围广泛，从传染病到神经科学靶点均有涉及。在这里，我们描述了一种从商业可得的起始原料制备吡咯并[1,2-α]喹喔啉酮的通用合成序列，并展示了其在制备潜在 κ 阿片受体拮抗剂中的应用。简要介绍和讨论了后一组化合物的生物学数据。
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