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  • Title: A straightforward synthetic approach for roxindole.
    Author: Lange JH, de Jong JC, Sanders HJ, Visser GM, Kruse CG.
    Journal: Bioorg Med Chem Lett; 1999 Apr 05; 9(7):1055-6. PubMed ID: 10230639.
    Abstract:
    A concise synthetic approach to the dopamine autoreceptor agonist roxindole 1 has been devised. The key step in the novel route is the addition of succinic anhydride to 5-methoxyindolylmagnesium bromide, which circumvents the cumbersome construction of the indole moiety - via the Japp Klingemann- Fischer indole methodology - in the original route. This novel route will enable a quick, multi-gram synthesis of roxindole from cheap starting materials.
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