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 suc cinic anhydride to 5-methoxyindolylmagnesium bromide, which circumvents the cumbersome construction of the indole moiety - via the Japp Klingemann- Fi scher indole methodology - in the original route. This novel route will ena ble a quick, multi-gram synthesis of roxindole from cheap starting material s. (C) 1999 Elsevier Science Ltd. All rights reserved.