Controlled derivatization of polyhalogenated quinolines utilizing selective cross-coupling reactions |
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Authors: | M Brad Nolt |
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Institution: | Department of Medicinal Chemistry, Technology Enabled Synthesis Group, Merck & Co., Inc., PO Box 4, West Point, PA 19486, United States |
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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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