Synthesis of Quinine‐Inspired Antimalarials by Ni‐Catalysed Cross Electrophile Coupling
Aggie Lawer,
Finlay P. Player,
Vicky M. Avery
et al.
Abstract:We describe the efficient synthesis of novel dehydroxyquinines by arylation of quincorine bromide using Ni‐catalysed cross electrophile coupling. The method demonstrates robust compatibility with (hetero)aryl bromides bearing diverse functional groups. Oxidation at C‐9 of the dehydroxyquinines expediently provided quinine‐inspired pseudo‐natural products (‘quinalogs’). Investigation of the compound collection against Plasmodium falciparum revealed a new insight into the structure activity relationship of quini… Show more
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