Facile Synthesis of 2-(4-Hydroxybiphenyl-3-yl)-1H-indoles from Anilines and 5′-Bromo-2′-hydroxyacetophenone

SYNTHETIC COMMUNICATIONS(2015)

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摘要
2-Arylindoles are attractive scaffolds because they are found in many pharmacologically active molecules. In this study, we describe the facile synthesis of diverse 2-(2-hydroxyphenyl)-1H-indoles from anilines and 5-bromo-2-hydroxyacetophenone in two steps using palladium-catalyzed indole cyclization as a key reaction. The indole cyclization was primarily controlled by the substituent properties of anilines. Suzuki-coupling reactions of 2-(5-bromo-2-hydroxyphenyl)-1H-indoles with arylboronic acids provided the corresponding 2-(4-hydroxybiphenyl-3-yl)-1H-indoles in moderate yield.
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关键词
2-Arylindoles,2-(4-hydroxybiphenyl-3-yl)-1H-indoles,indole cyclization
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