期刊
TETRAHEDRON
卷 70, 期 44, 页码 8413-8418出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tet.2014.07.092
关键词
Heterocycles; Cross-coupling; Palladium; Cyclization; Indazole
A set of variously substituted indazoles and hetero-aromatic derivatives were synthesized from o-halo-(het)arylaldehydes using a palladium catalyzed amination followed by cyclization. Starting from phenones, this process was extended to give 3-substituted indazoles. Moreover, N-1-substituted-indazoles can be reached by this strategy using an optional selective N-1-alkylation step during the process. This methodology offers a general and easy route for the synthesis of regioselectively substituted indazoles. (C) 2014 Elsevier Ltd. All rights reserved.
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