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3位未取代的中氮茚不仅具有多种重要的生物活性,且是重要的有机合成中间体.报道了一种从吡啶衍生物、氯乙酸和缺电子烯烃出发,在无过渡金属存在下合成3位未取代的中氮茚的新方法.该反应的关键步骤为四氢中氮茚中间体在2,2,6,6-四甲基哌啶氮氧自由基(TEMPO)存在下的氧化脱氢芳构化和脱羧反应.该反应操作简便,原料易得,且在反应中无需使用任何过渡金属试剂,具有一定的实用价值.
The 3-position unsubstituted indolizine not only has a variety of important biological activities, but also is an important intermediate for organic synthesis.A novel method for synthesizing indolizine from pyridine derivatives, chloroacetic acid and electron-deficient olefins has been reported in the absence of transition metal New method for unsubstituted 3-position indolizine The key step of this reaction is the oxidation of the tetrahydroindolizine intermediate in the presence of 2,2,6,6-tetramethylpiperidine nitroxide (TEMPO) Dehydroaromatization and decarboxylation reaction.The reaction is easy to operate, easy to get raw materials, and without any transition metal reagents in the reaction, has some practical value.