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通过铃木-宫浦交叉偶联反应合成甲基lycaconitine的5-取代环E类似物。

The synthesis of 5-substituted ring E analogs of methyllycaconitine via the Suzuki-Miyaura cross-coupling reaction.

作者信息

Huang Junfeng, Orac Crina M, McKay Susan, McKay Dennis B, Bergmeier Stephen C

机构信息

Department of Chemistry and Biochemistry, Ohio University, Clippinger Laboratories, Athens, OH 45701, USA.

出版信息

Bioorg Med Chem. 2008 Apr 1;16(7):3816-24. doi: 10.1016/j.bmc.2008.01.050. Epub 2008 Jan 31.

DOI:10.1016/j.bmc.2008.01.050
PMID:18272373
Abstract

Novel 3,5-disubstituted ring E analogs of methyllycaconitine were prepared and evaluated in nicotinic acetylcholine receptor binding assays. The desired analogs were prepared through the Suzuki-Miyaura cross-coupling reaction of methyl 5-bromo-nicotinate. The Suzuki-Miyaura cross-coupling reactions of pyridines with electron withdrawing substituents have not been extensively described previously.

摘要

制备了新型甲基lycaconitine的3,5-二取代环E类似物,并在烟碱型乙酰胆碱受体结合试验中进行了评估。所需类似物通过5-溴烟酸甲酯的铃木-宫浦交叉偶联反应制备。吡啶与吸电子取代基的铃木-宫浦交叉偶联反应此前尚未有广泛描述。

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引用本文的文献

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Defining the putative inhibitory site for a selective negative allosteric modulator of human α4β2 neuronal nicotinic receptors.定义人类 α4β2 神经元烟碱型乙酰胆碱受体选择性负变构调节剂的假定抑制部位。
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