摘要/Abstract

3-(2-氨基乙基)吡咯是形成6-氮杂吲哚骨架的重要中间体, 由于吡咯2位为高活性位点, 难以直接通过傅克反应合成3-(2-氨基乙基)吡咯. 报道了在吡咯α位引入拉电子基团, 形成对角β位的定位效应, 以无水AlCl₃为催化剂, 通过傅克反应在吡咯3位加成硝基烯烃, 进而得到取代的3-(2-氨基乙基)吡咯.
关键词: 三氯化铝, 3-(2-氨基乙基)吡咯, 6-氮杂吲哚
3-(2-Aminoethyl)pyrroles are important intermediates for the formation of the 6-azaindole skeleton. It was difficult
to synthesize 3-(2-aminoethyl)pyrroles from pyrrole by Friedel-Crafts alkylation directly because of the inactive site. The electron withdrawing groups were introduced at the α-position of pyrrole to form a positioning effect at the diagonal β-position. With anhydrous AlCl₃ as the catalyst, nitroalkenes could be added to the 3-position of pyrrole via Friedel-Crafts alkylation to obtain substituted 3-(2-aminoethyl)pyrroles.
Key words: Keywords aluminium chloride, 3-(2-aminoethyl)pyrrole, 6-azaindole


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