- Selective C-H trifluoromethylation of benzimidazoles through photoredox catalysis
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The protocol presented here is a new strategy for visible light induced C-H trifluoromethylation at C4 of benzimidazoles using Togni's reagent in the presence of fac-Ir(ppy)3. Its advantages are its operational simplicity, mild reaction conditions, low catalyst loading and wide substrate scope in which electron-withdrawing, electron-donating groups and different protecting groups are tolerated.
- Gao, Guo-Lin,Yang, Chao,Xia, Wujiong
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supporting information
p. 1041 - 1044
(2017/02/05)
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- Indium-mediated one-pot benzimidazole synthesis from 2-nitroanilines or 1,2-dinitroarenes with orthoesters
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One-pot reduction-triggered heterocyclizations from 2-nitroanilines or 1,2-dinitroarenes to benzimidazoles were investigated in this study. In the presence of indium/AcOH in ethyl acetate at reflux, reaction of 2-nitroanilines or 1,2-dinitroarenes with R-C(OMe)3 (R=Me, Ph) produced excellent yields of the corresponding benzimidazoles within 30 min to 6 h depending on the substituents of the starting materials. Indium-mediated heterocyclization of 2-nitroanilines to benzimidazole was faster and had better yields than 1,2-dinitroarenes to benzimidazole under similar reaction conditions.
- Kim, Jaeho,Kim, Jihye,Lee, Hyunseung,Lee, Byung Min,Kim, Byeong Hyo
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experimental part
p. 8027 - 8033
(2011/11/06)
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- 1-(3-Aryloxyaryl)benzimidazole sulfones are liver X receptor agonists
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A series of 1-(3-aryloxyaryl)benzimidazoles incorporating a sulfone substituent (6) was prepared. High affinity LXR ligands were identified (LXRβ binding IC50 values 10 nM), some with excellent agonist potency and efficacy in a functional assay of LXR activity measuring ABCA1 mRNA increases in human macrophage THP1 cells. The compounds were typically stable in liver microsome preparations and had good oral exposure in mice.
- Travins, Jeremy M.,Bernotas, Ronald C.,Kaufman, David H.,Quinet, Elaine,Nambi, Ponnal,Feingold, Irene,Huselton, Christine,Wilhelmsson, Anna,Goos-Nilsson, Annika,Wrobel, Jay
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scheme or table
p. 526 - 530
(2010/05/19)
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- BENZIMIDAZOLE COMPOUNDS
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This invention relates generally to benzimidazole-based modulators of Liver X receptors (LXRs) and related methods (Formula I). wherein R2 is C6-C10 aryl or heteroaryl including 5-10 atoms, each of which is: (i) substituted with 1 R7, and (ii) optionally substituted with from 1-5 Re; and R1, R3, R4, R5, R6, R7, and Re are defined herein.
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Page/Page column 83-84
(2009/08/14)
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