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A convenient and efficient protocol for the synthesis of thetetrazolo[1,5-a]quinoxalin-4(5H)-ones via copper-catalyzed [3+2] cyclization of azidotrimethylsilane with quinoxalin-2(1H)-ones under mild conditions has been disclosed. This practical protocol is compatible with a variety of functional groups and provides an access to functionalized tetrazolo[1,5-a]quinoxalin-4(5H)-ones from readily available and safe starting materials. (Figure presented.).

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The first example of oxidative C-H fluoroalkoxylation of quinoxalinones with fluoroalkyl alcohols under transition-metal and solvent-free conditions is described. This approach provides the synthesis of fluoroalkoxylated quinoxaline derivatives with good to excellent yields under mild reactions conditions. This method can also be extended to the facile and efficient synthesis of histamine-4 receptor.

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The synthesis method disclosed by the invention 3 – has the advantages of simple process, moderate. reaction conditions, moderate: yield, high yield and, the like, and the method has the, advantages, of, simple . process, mild reaction conditions, high yield and the like 3 . (by machine translation)

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A simple and efficient method for the visible light induced direct carbon alkylation of quinoxalin-2(1H)-ones at the C3 position is described. This protocol employs cheap and readily available phenyliodine(iii) dicarboxylates as the alkylation reagents to conduct decarboxylative radical coupling reaction with quinoxalin-2(1H)-ones. The process exhibits excellent compatibility to functional groups and provides a convenient and selective access to various 3-alkylquinoxalin-2(1H)-ones in good yields.

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Compounds of Formula (I) are useful for inhibition of Raf kinases. Methods of using compounds of Formula (I), stereoisomers, tautomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed

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An effective approach to realize the direct methylation of imidazo[1,2-a]pyridines and quinoxalin-2(1H)-ones with peroxides under metal-free conditions is described. In this protocol, peroxides serve as both the radical initiator and methyl source. Methylated imidazopyridines and quinoxalin-2(1H)-ones were smoothly synthesized in moderate to good yields. A free radical reaction mechanism was proposed to describe the methylation process.

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A novel visible-light-driven decarboxylative coupling of alkyl N-hydroxyphthalimide esters (NHP esters) with quinoxalin-2(1H)-ones has been developed. This C(sp2)?C(sp3) bond-forming transformation exhibits excellent substrate generality with respect to both the coupling partners. Of note, a series of 3-primary alkyl-substituted quinoxalin-2(1H)-ones that were difficult to synthesize by previous methods could be obtained in moderate to excellent yields. Additionally, the mild conditions, easy availability of substrates, wide functional group tolerance and operational simplicity make this protocol practical in the synthesis of 3-alkylated quinoxalin-2(1H)-ones.

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Disclosed herein is a direct C?H trifluoromethylation of quinoxalin-2(1H)-ones with sodium trifluoromethanesulfinate. This protocol affords a series of 3-trifluoromethylquinoxalin-2(1H)-one derivatives in moderate to excellent yields under transition-metal-free conditions. The present methodology features utilization of the inexpensive trifluoromethyl source without transition-metal-catalysts, mild reaction conditions and high functional group tolerance, which promises a convenient and efficient access to pharmaceutically interesting quinoxalinones. (Figure presented.).

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The first example of rapidly three-component cascade reaction of quinoxalinones with unactivated alkenes and TMSN3 under mild condition has been described. This approach provides a practical solution for the rapid modification of quinoxalinones and enables new planning strategies for the synthesis of bioactive organoazides. A radical mechanism is responsible for this three-component transformation.

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A practical and efficient synthetic route to construct a variety of 3-amidated quinoxalin-2(1H)-ones was developed via transition-metal free direct oxidative amidation of quinoxalin-2(1H)-ones with amidates using Selectfluor reagent as a mild oxidant. This protocol features mild reaction conditions, operational simplicity, broad substrate scope, and good to excellent yields.

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