The ring opening of 3,4-dichloro-1,2,5-thiadiazole with metal amides. A new synthesis of 3,4-disubstituted-1,2,5-thiadiazoles |
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| Authors: | Alain Merschaert Pascal Boquel Hugo Gorissen Jean-Pierre Van Hoeck Alfio Borghese Luc Antoine Vincent Mancuso Anne Mockel Michel Vanmarsenille |
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| Affiliation: | Lilly Research Laboratories, Chemical Product Research and Development, Rue Granbonpré 11, 1348 Mont-Saint-Guibert, Belgium |
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| Abstract: | We have developed a new synthesis of 3,4-disubstituted-1,2,5-thiadiazoles. The methodology is based on the ring opening of readily available 3,4-dichloro-1,2,5-thiadiazole with metal amides to afford a stable synthon, which is then transformed into the 3,4-disubstituted-1,2,5-thiadiazole derivatives via two consecutive reactions with O-, S-, N- or C-nucleophiles. |
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