A straightforward synthetic approach for roxindole

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.