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

The synthesis of 5-substituted ring E analogs of methyllycaconitine via the Suzuki-Miyaura cross-coupling reaction.
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通过 Suzuki-Miyaura 交叉偶联反应合成甲基乌头碱的 5-取代环 E 类似物。

DOI:
10.1016/j.bmc.2008.01.050
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发表时间:
2008
影响因子:
3.5
通讯作者:
Bergmeier,StephenC
Bergmeier,StephenC
中科院分区:
医学3区
文献类型:
--
作者:
Huang,Junfeng;Orac,CrinaM;McKay,Susan;McKay,DennisB;Bergmeier,StephenC

文献摘要

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合成了新的3,5-二取代环E甲基乌头碱类似物,并在烟碱型乙酰胆碱受体结合实验中进行了评价。通过5-溴烟酸甲酯的Suzuki-Miyaura交叉偶联反应制备了所需的类似物。吡啶与吸电子取代基的Suzuki-Miyaura交叉偶联反应以前没有被广泛描述过。
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.