5-溴-2-氯吡啶置于正丁基锂,二丁基镁,磺酰氯体系中,用 四氢呋喃,甲苯 作为反应溶剂,化学反应生成 2-氯吡啶-5-磺酰氯 参考文献:Efficient And Scalable Synthesis Of Pyridine Sulfonamides 标题:Efficient And Scalable Synthesis Of Pyridine Sulfonamides 摘要:短步长且可扩展的2,6-二溴吡啶转化为6-溴吡啶-2-磺酰胺的转化方法,通过卤素-金属交换和随后的磺酒氯反应再经酰胺化实现.该方法在合成各种吡啶磺酰胺中的应用也进行了描述. DOI:10.1055/s-0030-1259953
参考文献:10.1021/jm201091t 摘要:Brand S, Cleghorn LAT, McElroy SP, Robinson DA, Smith VC, Hallyburton I, Harrison JR, Norcross NR, Spinks D, Bayliss T, Norval S, Stojanovski L, Torrie LS, Frearson JA, Brenk R, Fairlamb AH, Ferguson MAJ, Read KD, Wyatt PG, Gilbert IH. Discovery of a Novel Class of Orally Active Trypanocidal N-Myristoyltransferase Inhibitors. J. Med. Chem. 2011 Dec 07;55(1):140–52. doi: 10.1021/jm201091t.