Journal
ORGANIC LETTERS
Volume 24, Issue 47, Pages 8703-8708Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.2c03630
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Funding
- Young Backbone Teachers Fund of Henan Province
- National Natural Science Foundation of China
- [2021GGJS012]
- [82130103]
- [U1804283]
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In this study, an intramolecular sp3 C-H amination reaction of aniline derivatives was established using molecular iodine under transition-metal-free conditions. The reaction yielded 1,2-fused or 1,2-disubstituted benzimidazoles in an efficient and scalable fashion. This synthetic process also produced novel benzimidazolium frameworks and bioactive compounds.
An intramolecular sp3 C-H amination reaction of aniline derivatives has been established. This reaction employs molecular iodine (I2) under transition-metal-free conditions and produces 1,2-fused or 1,2-disubstituted benzimidazoles. This opera-tionally simple synthetic process works well with N-substituted aniline substrates, forming novel benzimidazolium frameworks. Under the optimal reaction conditions, a broad variety of 1,2-fused/disubstituted benzimidazoles and benzimidazolium salts, including several bioactive compounds, were synthesized from readily accessible precursors in an efficient and scalable fashion.
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