Abstract
AbstractThe antimalarial [quinoline‐3‐14C]‐SSR97193 (ferroquine) (8), an analogue of chloroquine (CQ) (1), was synthesized from [2‐14C]‐malonic acid with an overall radiochemical yield of 15%. The synthetic route via [14C]‐Meldrum's acid (9) was designed to minimize the intermediacy of radiolabelled volatiles. This synthesis involves a four‐step route to labelled 4,7‐dichloroquinoline, which is the key intermediate for the synthesis of many analogues of CQ. Copyright © 2004 John Wiley & Sons, Ltd.
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