TsOH·H2O-Catalyzed Friedel-Crafts of Indoles of 3-Hydroxyisobenzofuran-1(3H)-One with Indoles: Highly Synthesis of 3-Indolyl-Substituted Phthalides


An efficient and facile method for the synthesis of 3-indolyl-substituted phthalides by Friedel-Crafts alkylation of indoles with 3-hydroxyisobenzofuran-1(3H)-one has been developed. Using only 2 mol-% TsOH·H2O as the catalyst, various substituted indoles can react smoothly at room temperature to give the corresponding phthalides products in good to excellent yields (up to 96%).

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H. Tang, X. Zhang, A. Song and Z. Zhang, "TsOH·H2O-Catalyzed Friedel-Crafts of Indoles of 3-Hydroxyisobenzofuran-1(3H)-One with Indoles: Highly Synthesis of 3-Indolyl-Substituted Phthalides," Modern Research in Catalysis, Vol. 1 No. 2, 2012, pp. 11-14. doi: 10.4236/mrc.2012.12002.

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The authors declare no conflicts of interest.


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