The synthesis of new, selected analogues of the pro-apoptotic and anticancer molecule HA 14-1

A new and versatile strategy has been developed towards HA 14-1 analogues, selectively modified on position 4 and/or on the primary amine function. An important aspect was the appropriate selection of the phenol protective group in the 5-bromosalicylaldehyde, allowing the isolation of the key intermediate the 2H-benzopyrane-2-imine 2′