Controlled derivatization of polyhalogenated quinolines utilizing selective cross-coupling reactions

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. (C) 2008 Elsevier Ltd. All rights reserved.