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Efficient Large-Scale Synthesis of 2-Amino-5-methanesulfonylaminobenzenesulfonamide |
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| Authors: | Peter S Dragovich Douglas E Murphy Chinh V Tran Frank Ruebsam |
| Institution: | 1. Anadys Pharmaceuticals, San Diego , California, USA pdragovich@anadyspharma.com;3. Anadys Pharmaceuticals, San Diego , California, USA |
| Abstract: | A novel synthesis of 2-amino-5-methanesulfonylaminobenzenesulfonamide is described. This preparation begins with readily available 4-nitroaniline and proceeds through five steps (isolations) in 41% overall yield. The described chemistry is conducted on a 50- to 100-g scale and does not require extractive workup procedures or chromatographic purifications. |
| Keywords: | 2-Amino-5-methanesulfonylaminobenzenesulfonamide Friedel–Crafts acylation Sulfonamide |