- Regioselective copper-diamine-catalyzed C-H arylation of 1,2,4-triazole ring with aryl bromides
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A convenient methodology for the regioselective C-H arylation of 1,2,4-triazole ring was developed. Using a benchtop stable Cu-diamine catalyst system, C-H functionalization of a simple 1,2,4-triazole substrate with various aryl bromides was regioselectively accomplished at the C5 position of the triazole ring.
- Jamal, Zaini,Teo, Yong-Chua
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p. 75449 - 75452
(2016/08/24)
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- C-H arylation and alkenylation of imidazoles by nickel catalysis: Solvent-accelerated imidazole C-H activation
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The first nickel-catalyzed C-H arylations and alkenylations of imidazoles with phenol and enol derivatives are described. Under the influence of Ni(OTf)2/dcype/K3PO4 (dcype: 1,2-bis(dicyclohexylphosphino)ethane) in t-amyl alcohol, imidazoles can undergo C-H arylation with phenol derivatives. The C-H arylation of imidazoles with chloroarenes as well as that of thiazoles and oxazoles with phenol derivatives can also be achieved with this catalytic system. By changing the ligand to dcypt (3,4-bis(dicyclohexylphosphino)thiophene), enol derivatives could also be employed as coupling partners achieving the C-H alkenylation of imidazoles as well as thiazoles and oxazoles. Thus, a range of C2-arylated and alkenylated azoles can be synthesized using this newly developed nickel-based catalytic system. The key to the success of the C-H coupling of imidazoles is the use of a tertiary alcohol as solvent. This also allows the use of an air-stable nickel(ii) salt as the catalyst precursor.
- Muto, Kei,Hatakeyama, Taito,Yamaguchi, Junichiro,Itami, Kenichiro
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p. 6792 - 6798
(2015/11/24)
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- MULTIHETEROARYL COMPOUNDS AS INHIBITORS OF H-PGDS AND THEIR USE FOR TREATING PROSTAGLANDIN D2 MEDIATED DISEASES
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Multiheteroaryl compounds, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical use in the prevention and treatment of prostaglandin D2 mediated diseases and conditions that may be modulated by the inhibition of hematopoietic prostaglandin D synthase (H-PGDS).
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Page/Page column 21
(2010/04/23)
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