Synthesis of Fused Polycyclic 1,4-Benzodiazepines via a Metal-Free Cascade Cyclization of 2-Acylbenzoic Acids with <i>N-</i>(<i>o</i>-Aminobenzyl)-indoles
An unprecedented metal-free cascade cyclization of 2-acylbenzoic acids with <i>N</i>-(2-aminobenzyl)-indoles was developed, which provided a powerful method for the construction of fused polycyclic skeleton. A variety of isoindoline/indole-fused 1,4-benzodiazepines were facilely obtained in moderate to good yields in one step. This protocol features good functional group tolerance, metal-free conditions, easy scalability and versatile transformations of products.
Authors
- Miao Tian (ORCID: https://orcid.org/0000-0002-1155-3220)
- Shukai Duan (ORCID: https://orcid.org/0000-0002-0040-3796)
- Kai Sun (ORCID: https://orcid.org/0000-0002-0041-6044)
- Xin‐Ming Xu (ORCID: https://orcid.org/0000-0002-3015-9050)
- Qian Liu (ORCID: https://orcid.org/0000-0003-1692-3267)
- Zhongyuan Zhao (ORCID: https://orcid.org/0000-0002-8787-8267)
- Zu‐Li Wang (ORCID: https://orcid.org/0000-0002-3503-4097)
Institutions
- Qingdao Agricultural University (CN)
- Nanjing Forestry University (CN)
- Yantai University (CN)
- Pharmaceutical Biotechnology (Czechia) (CZ)
Publication Details
- Journal
- The Journal of Organic Chemistry
- Published
- 2025-09-27
- DOI
- https://doi.org/10.1021/acs.joc.5c01615
- Primary Topic
- Synthesis and pharmacology of benzodiazepine derivatives
- Type
- article
- Field-Weighted Citation Impact
- 0.00