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Ultrasound-assisted bromination of indazoles at the C3 position with dibromohydantoin
Bromoaryl compounds have attracted great attention in organic chemistry, especially for the synthesis of pharmaceutical intermediates. Herein, we demonstrated a novel and efficient bromination protocol of indazoles via C–H bond cleavage to give site-specific 3-bromide products that could be further...
Autores principales: | , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
The Royal Society of Chemistry
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9773018/ https://www.ncbi.nlm.nih.gov/pubmed/36605629 http://dx.doi.org/10.1039/d2ra06867b |
Sumario: | Bromoaryl compounds have attracted great attention in organic chemistry, especially for the synthesis of pharmaceutical intermediates. Herein, we demonstrated a novel and efficient bromination protocol of indazoles via C–H bond cleavage to give site-specific 3-bromide products that could be further employed as synthetic blocks to prepare drugs. The reaction used DBDMH as a bromine source, tolerated a wide range of indazoles, and finished in 30 min under mild, ultrasound-assisted conditions. Besides, preliminary mechanistic studies revealed that this approach was not a radical process. |
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