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Chemistry of Heterocyclic Compounds

, Volume 54, Issue 3, pp 334–338 | Cite as

Activation-free one-pot alkynylation–cyclization synthesis of 2-substituted 4-azaindoles and indoles

  • Timo Lessing
  • Thomas J. J. MüllerEmail author
Article

2-Substituted 4-azaindoles and indoles are rapidly and efficiently prepared in an activation-free Pd-catalyzed alkynylation–cyclization sequence starting from 3-amino-2-bromopyridine or o-bromoaniline and terminal alkynes in a one-pot fashion.

Keywords

4-azaindoles heterocycles indoles alkynylation cyclization one-pot reaction 

Notes

The authors cordially thank the Fonds der Chemischen Industrie for financial support (scholarship for Timo Lessing).

The authors cordially thank the microanalytical laboratory of the Institut für Medizinische und Pharmazeutische Chemie at the Heinrich-Heine-Universität Düsseldorf for the elemental analyses measurment.

Supplementary material

10593_2018_2269_MOESM1_ESM.pdf (1.3 mb)
ESM 1 (PDF 1290 kb)

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Copyright information

© Springer Science+Business Media, LLC, part of Springer Nature 2018

Authors and Affiliations

  1. 1.Institut für Organische Chemie und Makromolekulare Chemie, Lehrstuhl für Organische ChemieHeinrich-Heine-Universität DüsseldorfDüsseldorfGermany

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