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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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Efficient synthesis of 2,4-disubstituted 1,2,4-benzothiadiazin-3-one 1,1-dioxides on solid support.

The first solid-phase synthesis of 1,2,4-benzothiadiazin-3-one 1,1-dioxides has been developed. Synthesis of the title compounds was achieved by the reduction of 2-nitrobenzenesulfonamides, followed by cyclization with carbonyldiimidazole. Because 1,2,4-benzothiadiazin-3-one 1,1-dioxides have been known to possess various bioactivities, this method is useful from the viewpoint of new drug discovery. In addition to the excellent purity of the title compounds, a large number of compounds can be synthesized with this method, because this synthesis includes four diversity points.[1]

References

  1. Efficient synthesis of 2,4-disubstituted 1,2,4-benzothiadiazin-3-one 1,1-dioxides on solid support. Makino, S., Nakanishi, E., Tsuji, T. Journal of combinatorial chemistry. (2003) [Pubmed]
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