Journal
TETRAHEDRON
Volume 63, Issue 9, Pages 1970-1980Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tet.2006.12.068
Keywords
azoles; direct arylation; regioselectivity; biologically active; compounds; C-H bond activation
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The Pd- and Cu-mediated reaction of a large variety of pi-electron sufficient heteroarenes, which include free (NH)-imidazoles, -benzimidazole and -indole, with aryl iodides under ligandless and base-free conditions provides regioselectively the required 2-arylhetero-cycle derivatives in high yields. 2-Aryl-1-phenyl-1H-imidazoles can also be prepared by a one-pot domino HALEX and Pd- and Cu-mediated arylation reactions of 1-phenyl-1H-imidazole with activated and unactivated aryl bromides under base-free and ligandless conditions. The protocol for the synthesis of 2-arylazoles involving the use of aryl iodides has been found to be suitable for the efficient preparation of three bioactive compounds and a key intermediate in the synthesis of a heparanase inhibitor. (c) 2007 Elsevier Ltd. All rights reserved.
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