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Org Lett. 2008 Dec 4;10(23):5353-6. doi: 10.1021/ol802145b.
The first total synthesis of the natural product 3-hydroxy-11-norcytisine (1), structurally related to cytisine (2), a benchmark ligand at neuronal nicotinic acetylcholine receptors (NNRs), has been achieved. The synthesis permits the unambiguous confirmation of the structure originally proposed for 1 and has enabled initial biological characterization of 1 and its related compounds against NNRs.
天然产物 3-羟基-11-去甲野靛碱(1)的全合成首次实现,其结构与烟碱(2)有关,后者是神经元烟碱型乙酰胆碱受体(NNR)的基准配体。该合成方法能够明确确认最初为 1 提出的结构,并使 1 及其相关化合物对 NNR 的初步生物学特性得以表征。