Solid-phase synthesis of tetrasubstituted 2-imino-1,3-thiazolines using a functionalizing cleavage strategy |
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| Authors: | Laurent Gomez,Franç oise Gellibert,Charles Mioskowski |
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| Affiliation: | a Université Louis Pasteur, Laboratoire de Synthèse BioOrganique, CNRS, 74 Route du Rhin, 67401 Illkirch, France
b GlaxoSmithKline, 25-27 Avenue du Quebec, 91951 Les Ullis, France |
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| Abstract: | A novel solid-phase synthesis of tetrasubstituted 2-imino-1,3-thiazolines using a functionalizing cleavage strategy is described. The synthetic route utilized the ambident reactivity of a dithiocarbamate functionality to synthesize the key resin-bound electrophilic thiazolium intermediate. The desired products were efficiently obtained in high purity by the reaction of various amines with the thiazolium salt. |
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