Huang Junfeng, Orac Crina M, McKay Susan, McKay Dennis B, Bergmeier Stephen C
Department of Chemistry and Biochemistry, Ohio University, Clippinger Laboratories, Athens, OH 45701, USA.
Bioorg Med Chem. 2008 Apr 1;16(7):3816-24. doi: 10.1016/j.bmc.2008.01.050. Epub 2008 Jan 31.
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.
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。