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ACID-CATALYZED ADDITION OF N-HYDROXYUREA TO 1-ARYL ALCOHOL DERIVATIVES: A NEW SYNTHESIS OF ZILEUTON |
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| Abstract: | A highly efficient synthesis of Zileuton is described in which the key step involves a site-specific alkylation of hydroxyurea under acid catalysis. Various aryl alcohol electrophiles were tested and the reaction was found to be highly substrate-specific, favoring benzothiophene and benzofuran-based alcohols. |
| Keywords: | Alkylation Hydroxamic Acids and Derivatives Regioselection |