Methods for the synthesis of indole-3-carboxylic acid esters (microreview)

In this microreview, recent advances in the development of methods for indole cyclization, leading to indole-3-carboxylic acid derivatives, are highlighted. Selected works published since 2013 are covered.

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  1. 1.

    Chadha, N.; Silakari, O. Eur. J. Med. Chem. 2017, 134, 159.

  2. 2.

    (a) Shchekotikhin, A. E.; Glazunova, V. A.; Dezhenkova, L. G.; Luzikov, Y. N.; Buyanov, V. V.; Treshalina, H. M.; Lesnaya, N. A.; Romanenko, V. I.; Kaluzhny, D. N.; Balzarini, J.; Agama, K.; Pommier, Y.; Shtil, A. A.; Preobrazhenskaya, M. N. Eur. J. Med. Chem. 2014 , 86, 797. (b) Tikhomirov, A. S.; Litvinova, V. A.; Luzikov, Y. N.; Korolev, A. M.; Sinkevich, Y. B.; Shchekotikhin, A. E. Chem. Heterocycl. Compd. 2017, 53, 1072. [Khim. Geterotsikl. Soedin. 2017, 53, 1072.]

  3. 3.

    Liu, X.-G.; Li, Z.-H.; Xie, J.-W.; Liu, Р.; Zhang, J.; Dai, В. Tetrahedron 2016, 72, 653.

  4. 4.

    Shen, D.; Han, J.; Chen, J.; Deng, H.; Shao, М.; Zhang, Н.; Cao, W. Org. Lett. 2015, 17, 3283.

  5. 5.

    Li, H.; Zhao, Y.; Ma, L.; Ma, M.; Jiang, J.; Wan, X. Chem. Commun. 2017, 53, 5993.

  6. 6.

    (a) Lv, H.; Shi, J.; Wu, В.; Guo, Y.; Huang, J.; Yi, W. Org. Biomol. Chem. 2017, 15, 8054. (b) Li, Y.; Li, J.; Wu, Х.; Zhou, Y.; Liu, H. J. Org. Chem 2017, 82, 8984. (c) Mishra, N. K.; Choi, М.; Jo, Н.; Oh, Y.; Sharma, S.; Han, S. H.; Jeong, T.; Han, S.; Lee, S.-Y.; Kim, I. S. Chem. Commun. 2015, 51, 17229. (d) Li, Y.; Qi, Z.; Wang, Н.; Yang, Х.; Li, X. Angew. Chem., Int. Ed. 2016, 55, 11877. (e) Jiang, H.; Gao, Sh.; Xu, J.; Wu, Х.; Lin, А.; Yao, Н. Adv. Synth. Catal. 2016, 358, 188. (f) Shi, P.; Wang, L.; Guo, S.; Chen, K.; Wang, J.; Zhu, J. Org. Lett. 2017, 19, 4359. (g) Patel, P.; Borah, G. Eur. J. Org. Chem. 2017, 2272.

  7. 7.

    Nguyen, H. H.; Kurth, M. J. Org. Lett. 2013, 15, 362.

  8. 8.

    Lian, X.-L.; Ren, Zh.-H.; Wang, Y.-Y.; Guan, Zh.-H. Org. Lett. 2014, 16, 3360.

  9. 9.

    (a) Zoller, J.; Fabry, D. C.; Ronge, M. A.; Rueping, M. Angew. Chem., Int. Ed. 2014, 53, 13264. (b) Wu, Ch.-J.; Meng, Q.; Lei, T.; Zhong, J.-J.; Liu, W.-Q.; Zhao, L.-M.; Li, Zh.-J.; Chen, B.; Tung, Ch.-H.; Wu, L.-Zh. ACS Catal. 2016, 6, 4635. (c) Liu, W.-Q.; Lei, Т.; Song, Z.-Q.; Yang, X.-L.; Wu, Ch.-J.; Jiang, X.; Chen, B.; Tung, Сh.-H.; Wu, L.-Zh. Org. Lett. 2017, 19, 3251.

  10. 10.

    Festa, A. Chem. Heterocycl. Compd. 2018, 54, 22. [Khim. Geterotsikl. Soedin. 2018, 54, 22.]

  11. 11.

    Tang, S.; Gao, X.; Lei, A. Chem. Commun. 2017, 53, 3354.

  12. 12.

    Gharpure, S. J.; Anuradha, D. Org. Lett. 2017, 19, 6136.

  13. 13.

    Bodunov, V. A.; Galenko, Е. Е.; Galenko, A. V.; Novikov, M. S.; Khlebnikov, A. F. Synthesis 2018, 2784.

  14. 14.

    Jiang, M.; Xiang, H.; Zhu, F.; Xu, X.; Deng, L.; Yang, C. Org. Biomol. Chem. 2015, 13, 10122.

  15. 15.

    Formenti, D.; Ferretti, F.; Ragaini, F. ChemCatChem 2018, 10, 148.

  16. 16.

    Baumann, M.; Baxendale, I. R.; Deplante, F. Beilstein J. Org. Chem. 2017, 13, 2549.

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The material was prepared with the partial support of the Grants Council of the President of the Russian Federation for state support of young Russian scientists (grant МК-2474.2018.3)

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Correspondence to Alexander S. Tikhomirov.

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Translated from Khimiya Geterotsiklicheskikh Soedinenii, 2018, 54(10), 923–925

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Litvinova, V.A., Tikhomirov, A.S. Methods for the synthesis of indole-3-carboxylic acid esters (microreview). Chem Heterocycl Comp 54, 923–925 (2018).

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