Abstract
AbstractThe first example on the C5, C7‐dihalogenation of 8‐hydroxyquinolines based on an in situ O‐acyl 8‐hydroxyquinoline formation is realized under catalyst‐free condition in toluene. Modifying the reaction conditions by directly utilizing O‐acylated 8‐hydroxyquinolines in the presence of AlCl3 enables the electrophilic halogenation in the C5 position, leading to the tunable synthesis of C5 halogenated products. The O‐acyl group can be easily removed from the product to provide halogenated quinolines containing free hydroxyl group by simple hydrolysis.
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