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研究实现了高对映选择性的硝基烷烃对N-Boc靛红亚胺1的不对称aza-Henry反应,来构建胺基季碳氧化吲哚.发现在金鸡纳碱衍生的叔胺-酚羟基双功能催化剂C5的作用下,10种不同取代的N-Boc靛红亚胺与硝基甲烷的反应均能顺利进行,以66%~91%的对映选择性得到目标产物,产物的绝对构型通过X-ray单晶衍射加以确定.硝基乙烷和硝基丙烷也能高对映选择性地参与反应,但非对映选择性不佳.
The asymmetric aza-Henry reaction of highly enantioselective nitroalkanes with N-Boc isocyanurate 1 was studied to construct the amino quaternary carbon oxido-indoles. It was found that in the case of cinchona-derived tertiary amine-phenol Reaction of 10 different substituted N-Boc isophthalimines with nitromethane can be carried out smoothly under the action of C5 bifunctional catalyst C5, and the target product is obtained with the enantioselectivity of 66% -91%. The absolute The configuration was confirmed by X-ray single crystal diffraction. Nitroethane and nitropropane were also able to participate in the reaction with high enantioselectivity but with poor diastereoselectivity.