Metal‐Free Oxidative Annulation toward an Ultrathermostable Nitrogen‐Rich Fused Azaarene
The development of nitrogen-rich fused azaarenes with exceptional thermal stability remains a critical challenge because the incorporation of high-energy N─N and N═N linkages typically compromises molecular stability. Herein, we report a metal-free oxidative annulation strategy for the construction of an ultrathermostable pyrazole-fused azaarene (TYX-40) through concurrent N═N and C─C bond formation from a simple aminopyrazole precursor. Using hydrogen peroxide as a green oxidant under mild conditions, this transformation enables direct self-coupling of 3,5-diamino-1H-pyrazole to furnish a highly conjugated [5,6,5]-fused nitrogen-rich framework (TYX-40) without transition-metal catalysis. Mechanistic investigations, including radical-trapping experiments and density functional theory calculations, support a radical-mediated sequential annulation pathway involving oxidative azo formation followed by intramolecular C─C coupling. Benefiting from its highly planar and symmetric fused-ring architecture, TYX-40 exhibits exceptional thermal stability with a decomposition temperature of 414°C, among the highest values reported for nitrogen-rich fused heterocycles. Computational analyses reveal that enhanced aromatic delocalization and uniform electronic distribution play critical roles in stabilizing the fused azaarene framework.
Authors
- Guangbin Cheng (ORCID: https://orcid.org/0000-0003-0501-6469)
- Yuji Liu (ORCID: https://orcid.org/0000-0003-2558-5896)
- Wei Huang (ORCID: https://orcid.org/0000-0002-4376-4639)
- Yongxing Tang (ORCID: https://orcid.org/0000-0002-9549-9195)
- Zhiwei Zeng (ORCID: https://orcid.org/0000-0002-2285-896X)
- Peng‐Fei Cui (ORCID: https://orcid.org/0009-0001-8104-8617)
- Chunhui Chen
- Mingjie Tang
- Jing Liu
- Chuan Xiao
Institutions
- China North Industries Group Corporation (China) (CN)
- China South Industries Group (China) (CN)
- Nanjing University of Science and Technology (CN)
Publication Details
- Journal
- Small
- Published
- 2026-08-27
- DOI
- https://doi.org/10.1002/smll.75521
- Primary Topic
- Catalytic C–H Functionalization Methods
- Type
- article
- Field-Weighted Citation Impact
- 0.00
Funders
- National Natural Science Foundation of China
- Government of Jiangsu Province
- Natural Science Foundation of Jiangsu Province
- Nanjing University of Science and Technology
- Nanjing University