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Controlled derivatization of polyhalogenated quinolines utilizing selective cross-coupling reactions
Authors:M Brad Nolt
Institution:Department of Medicinal Chemistry, Technology Enabled Synthesis Group, Merck & Co., Inc., PO Box 4, West Point, PA 19486, United States
Abstract:Straightforward procedures for the derivatization of tri- and tetrahalogenated quinolines utilizing sequential selective Pd-catalyzed cross-coupling reactions are described. Taking advantage of intrinsic halide reactivity, substrate control, and appropriate reaction conditions, highly selective reactions at the quinoline 3-, 4-, and 6-position are possible.
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