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| N-alkylsulfonamides is a class of biologically active compounds such as antibacterial, anticancer, antiviral functions, and many classical N-alkylsulfonamides synthetic methods which involved sulfonyl halides with amines, sulfonamide with alcohol were reported successively. In this paper, TiCl4-mediated intermolecular or intramolecular direct N-alkylation reaction of sulfonamides with inactive ethers as alkylating agents was successfully achieved, and the effects of sulfonamides substrate, the kinds of Lewis acid, solvents, reaction time and reaction temperature etc. on the N-Alkylation were systematically investigated. This method provides a novel approach to make N-alkylsulfonamides from inactive ethers via an easy work-up procedure, this is the first report N-alkylation of sulfonamides using inactive ethers as alkylating reagents. |
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| Keywords:N-alkylation ; Lewis acid; N-alkylsulfonamide ; Di-alkyl ether ; Titanium tetrachloride |
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