Regioselective Pd-catalyzed indolization of 2-bromoanilines with internal alkynes using phosphine-free ligands |
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| Authors: | Xin Cui Yao Fu Qing-Xiang Guo |
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| Affiliation: | a Department of Chemistry, Joint Laboratory of Green Synthetic Chemistry, University of Science and Technology of China, Hefei 230026, China
b Department of Chemistry, Tsinghua University, Beijing 100084, China |
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| Abstract: | The possibility of using phosphine-free ligands to promote Pd-catalyzed indolization of 2-bromoanilines with internal alkynes was examined for the first time. Phenylurea was found to be the optimal ligand, which could mediate the synthesis of 2,3-disubstituted indoles in good yields (ca. 60-85%) with high regioselectivity. |
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| Keywords: | Indole Larock indolization Palladium catalyst Phosphine-free ligand Heteroannulation |
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