A straightforward synthetic approach for roxindole

JHM Lange, JC de Jong, HJ Sanders, GM Visser…

Index: Lange, Jos H. M.; De Jong, Johannes C.; Sanders, Hans J.; Visser, Geb M.; Kruse, Chris G. Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 7 p. 1055 - 1056

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Citation Number: 2

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 ...