4.7 Article

Efficient synthesis of 2-substituted indoles based on palladium(II) acetate/tri-tert-butylphosphine-catalyzed alkynylation/amination of 1,2-dihalobenzenes

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ADVANCED SYNTHESIS & CATALYSIS
卷 348, 期 7-8, 页码 846-850

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WILEY-V C H VERLAG GMBH
DOI: 10.1002/adsc.200606022

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alkynylation; amination; 1,2-dihalobenzenes; indoles; palladium; phosphane ligands

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A simple, efficient palladium(II) acetate/tri-tert-butylphosphine-catalyzed indole synthesis from o-alkynylhalobenzenes, readily available from 1,2-dihalobenzenes, has been achieved in good to excellent yields. A one-pot, Pd(OAc)(2)/t-Bu3P-catalyzed sequential reaction from 1-chloro-2-iodobenzene, phenylacetylene and amines has also been achieved in good yields.

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