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A Convenient Synthetic Approach to Saccharin Derivatives ­Containing a Sulfonylamidine Scaffold

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A key intermediate was obtained as solid through filtration of the reaction mixture of saccharin, chloro(triphenyl)phosphonium chloride, and N,N-diisopropylethylamine (DIPEA) in chloroform. The soluble triphenylphosphine oxide went to filtrate as… Click to show full abstract

A key intermediate was obtained as solid through filtration of the reaction mixture of saccharin, chloro(triphenyl)phosphonium chloride, and N,N-diisopropylethylamine (DIPEA) in chloroform. The soluble triphenylphosphine oxide went to filtrate as waste, while the solid was reacted with amines to afford N-sulfonylamidines. In total, 26 N-sulfonylamidine products were obtained in moderate to good overall yields.

Keywords: saccharin; sulfonylamidine; saccharin derivatives; convenient synthetic; approach saccharin; synthetic approach

Journal Title: Synthesis
Year Published: 2018

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