Novel methods for the synthesis of 5-substituted-3-carboxy-2,5- and 4,5-dihydrothiophenes and 5-substituted 2- and 3-sulfolenes |
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| Authors: | James A Wilkinson Nicolas Ardes-Guisot John Leonard |
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| Institution: | a Centre for Drug Design, Biosciences Research Institute, Cockcroft Building, University of Salford, Salford M5 4WT, UK
b AstraZeneca Process R+D, Silk Road, Macclesfield, Cheshire SK10 2NG, UK |
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| Abstract: | Various approaches to the syntheses of 5-substituted-3-carbomethoxy-2,5-dihydrothiophenes and their product sulfolenes, required as synthetic precursors for tangutorine, are described. An efficient route to 3,5-disubstituted-4,5-dihydrothiophenes and hence 3,5-disubstituted-2-sulfolenes by radical chemistry is also described. |
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| Keywords: | Sulfolene Dihydrothiophene Xanthate radical transfer |
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