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A general synthesis of 4-alkyl/aryl substituted saccharins |
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| Authors: | Chakrapani Subramanyam and Malcom R Bell |
| Institution: | Department of Medicinal Chemistry Sterling Winthrop Pharmaceutical Research Division, 81 Columbia Turnpike, Rensselaer, N.Y. 12144 U.S.A. |
| Abstract: | A new method for the synthesis of 4-alky/aryl substituted saccharins (2) has been developed. The key steps include conjugate addition/acylation of cyclohexenone (3) and reaction of the resulting β-ketoesters 4 with benzyl mercaptan to give the vinyl sulfides 5 and 6. The latter were converted to the saccharins 2 in high yield. |
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