- Direct Access to Halogenated Fused Imidazo[1,5-a]N-heteroaromatics through Copper-Promoted Double Oxidative C–H Amination and Halogenation
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An aerobic copper-promoted double oxidative C–H amination and halogenation tandem reaction of 2-methylazarenes with aliphatic amines or amino acids has been developed. The reaction uses copper salts as catalysts as well as halogen sources, and molecular oxygen as the sole oxidant. This protocol is operationally simple, and gives direct access to functionalised fused imidazoles in a one-pot operation with good functional-group tolerance. The synthetic utility of the products has been tested in a Suzuki cross-coupling reaction, which proceeded in good yield.
- Sandeep, Mummadi,Swati Dushyant, Patil,Sravani, Boda,Rajender Reddy, Kallu
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p. 3036 - 3047
(2018/06/27)
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- Aerobic Copper-Catalyzed Halocyclization of Methyl N-Heteroaromatics with Aliphatic Amines: Access to Functionalized Imidazo-Fused N-Heterocycles
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A new aerobic copper-catalyzed halocyclization reaction of methyl N-heteroaromatics and aliphatic amines has been developed, which enables straightforward access to functionalized imidazo-fused N-heterocycles with the merits of good functional tolerance, use of easily available copper salts as the catalysts, lithium halides as the halogen sources, and O2 as a sole oxidant. Due to the reaction features' selective introduction of halogen functionalities to the newly formed imidazo ring, further extensions of the developed chemistry toward synthetic diversity, including effective access to functional materials, are easily envisioned.
- Tan, Zhenda,Zhao, He,Zhou, Changjian,Jiang, Huanfeng,Zhang, Min
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p. 9939 - 9946
(2016/11/02)
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- Synthesis of quinoline coupled [1,2,3]-triazoles as a promising class of anti-tuberculosis agents
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A series of quinoline coupled 1,2,3-triazoles compounds have been synthesized by 'click chemistry' from azidomethyl quinoline with different alkynes. The efficiency and fidelity of the Cu(I)-catalyzed azide-alkyne reaction are substantiated by good yields and exclusive formation of the expected 1,4-disubstituted triazole product. All the synthesized compounds were screened for anti-tubercular activity against Mycobacterium tuberculosis H37Rv by luciferase reporter phage (LRP) assay. Quinoline coupled triazole sugar hybrid, 20 is the most potent compound in the series with 76.41% and 78.37% reduction calculated based on percentage reduction in Relative Light Units at 5 and 25 μg/mL, respectively.
- Karthik Kumar,Prabu Seenivasan,Kumar, Vanaja,Mohan Das
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p. 2084 - 2090
(2011/11/06)
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