Cu-Mediated Amination of (Hetero)aryl C-H bonds with NH Azaheterocycles.
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ID: 64006
2019
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Abstract
The direct synthesis of N -(hetero)arylated heteroarenes has been realized via Cu-mediated C-N coupling of NH azaheterocycles with aryl C-H bonds under aerobic conditions. This protocol features a broad scope of both heterocyclic arenes (pyridine, quinoline, pyrazole, imidazole, furan, thiophene, benzofuran, and indole) and NH azaheterocycles (imidazole, pyrazole, indole, azindole, purine, indazole, benzimidazole, pyridone, carbazole), providing a versatile method for the synthesis of pharmaceutically important N -(hetero)arylated heteroarenes. The versatility of this reaction was further demonstrated by late-stage modification of marketed drugs, and by synthesis of a key intermediate for accessing a class of Angiotensin II receptor 1 antagonists.
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yu2019cumediatedangewandte
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| Authors | Yu, Jin-Feng;Li, Jian-Jun;Wang, Peng;Yu, Jin-Quan; |
| Journal | angewandte chemie (international ed in english) |
| Year | 2019 |
| DOI |
10.1002/anie.201910395
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