Abstract
AbstractThe use of flow chemistry to obtain (7‐aza)indole derivatives was investigated in three steps (C‐3 iodination followed by N‐Boc protection). Excellent yields were achieved after very short reaction times. The challenge of using a continuous flow process was incremented by performing a novel copper‐free Sonogashira cross coupling in C‐3 (7‐Aza)indolic position using a recyclable supported palladium catalyst. A library of polyfunctionalized (7‐aza)indoles was obtained in high yield with a very efficient process (< 3 min.). Scale‐up was studied and the preparation of significant amounts of final alkynyl and Boc protected (aza)indoles can be immediately extended to a pilot scale in optimum security conditions.
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