Institute of Fine Chemistry and Engineering, College of Chemistry and Chemical Engineering, Henan University , Kaifeng 475004, China.
J Org Chem. 2017 Jun 2;82(11):5669-5677. doi: 10.1021/acs.joc.7b00488. Epub 2017 May 10.
An efficient Cu(OTf)-catalyzed Friedel-Crafts alkylation/cyclizaiton sequence of 3-substituted indoles with isatin-derived oxodienes was developed, and a series of structurally complex and diverse pyrrolo[1,2-a]indole spirooxindoles were first obtained in up to 99% yields. This protocol proved to be quite general and was also robust for the synthesis of 9H-pyrrolo[1,2-a]indoles.
发展了一种高效的三取代吲哚与色酮衍生的氧二烯的 Friedel-Crafts 烷基化/环化序列,首次通过该序列以高达 99%的收率得到了一系列结构复杂多样的吡咯并[1,2-a]吲哚螺环氧化吲哚。该方法具有广泛的适用性,对于 9H-吡咯并[1,2-a]吲哚的合成也具有很好的稳健性。