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Peer-reviewedCC BYOrganic letters

Direct C1-H Amination of Free NH Carbazoles Enabled by the Catellani Reaction.

  1. 1SynCat Lab, Department of Chemistry, Life Sciences and Environmental Sustainability, University of Parma, Parco Area delle Scienze 17/A, 43124Parma (PR), Italy.
  2. 2Department of Chemistry, Life Sciences and Environmental Sustainability, University of Parma, Parco Area delle Scienze 17/A, 43124Parma (PR), Italy.

Abstract

Carbazoles are valuable building blocks for emerging pharmaceuticals and bioactive compounds. However, methods to access C1-H-aminated carbazoles remain underdeveloped. Current approaches often require multistep syntheses or the use of toxic metals. Herein, we report the first Pd/NBE-catalyzed C1-H amination of NH-free carbazoles. The method introduces a broad range of cyclic amines onto carbazole scaffold and tolerates several functional groups, including acyl, pivaloyl, and halogen substituents. This approach expands the scope of the Catellani reactions to the direct amination of unprotected carbazoles, offering a concise entry to otherwise challenging C1-aminated scaffolds.

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BibTeX
@article{sorabad2026direct,
  title = {{Direct C1-H Amination of Free NH Carbazoles Enabled by the Catellani Reaction.}},
  author = {Ganesh Shivayogappa Sorabad and Paolo Pio Mazzeo and Elena Motti and Nicola Della Ca'},
  journal = {Organic letters},
  year = {2026},
  month = oct,
  doi = {10.1021/acs.orglett.6c03473},
  url = {https://europepmc.org/article/MED/42917815},
  note = {CC BY},
}
RIS
TY  - JOUR
TI  - Direct C1-H Amination of Free NH Carbazoles Enabled by the Catellani Reaction.
AU  - Ganesh Shivayogappa Sorabad
AU  - Paolo Pio Mazzeo
AU  - Elena Motti
AU  - Nicola Della Ca'
PY  - 2026
DA  - 2026/10/01
JO  - Organic letters
DO  - 10.1021/acs.orglett.6c03473
UR  - https://europepmc.org/article/MED/42917815
AB  - Carbazoles are valuable building blocks for emerging pharmaceuticals and bioactive compounds. However, methods to access C1-H-aminated carbazoles remain underdeveloped. Current approaches often require multistep syntheses or the use of toxic metals. Herein, we report the first Pd/NBE-catalyzed C1-H amination of NH-free carbazoles. The method introduces a broad range of cyclic amines onto carbazole scaffold and tolerates several functional groups, including acyl, pivaloyl, and halogen substituents. This approach expands the scope of the Catellani reactions to the direct amination of unprotected carbazoles, offering a concise entry to otherwise challenging C1-aminated scaffolds.
SN  - 1523-7060
SN  - 1523-7052
ER  -