Abstract: 2-Butyl-6-nitroindole was synthesized via the stepwise Pd-catalyzed cross-coupling of a triflate with hexyne starting from 2-amino-4-nitrophenol，where the amino group was protected by trifluoroacetic group. The triflate was obtained from the reaction of N-(2-hydroxy-4-nitrophenyl) trifluoroacetamide with PhNTf2 catalyzed by NaH. Structure of the product in each steps was checked and determined by IR，1H NRM，13C NMR and MS.

摘要： 介绍了一步关环合成2-丁基-6-硝基吲哚的新方法。室温氮气保护下，2-氨基-4硝基苯酚与三氟乙酰酐反应进行氨基保护，得到的2-（N-三氟甲基乙酰基）氨基-4-硝基苯酚与N-苯基双（三氟甲烷磺酰）亚胺（PhNTf2）在强碱 NaH作用下，生成三氟甲基磺酸酯，收率82.6%。之后，70～80 ℃氮气保护下，Pd(PPh3)4催化剂作用，与正己炔一步关环合成2-丁基-6-硝基吲哚，收率33.3%。产物结构经红外光谱、核磁共振和质谱检测并证实。将目标产物进行单晶培养，经单晶X衍射检测表征，阐明了结构。