Palladium-catalyzed heteroannulation of 2-ARYL- 3-IODO-4-(Phenylamino)quinolines and 4-(N,N-allylphenylamino)-2-ARYL-3-iodoquinolines

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Lesenyeho, Lehlogonolo Godfrey

Issue Date

2010-09

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Dissertation

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en

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2-Aryl-3-iodo-4-(phenylamino)quinoline , Sonogashira cross-coupling reaction , 4-(N,N-allylphenylamino)-2-aryl-3- iodoquinolines , intramolecular Heck reaction , 1H-pyrrolo[3,2-c]quinolines

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Abstract

The previously described 2-aryl-4-chloro-3-iodoquinolines were prepared following literature procedure and in turn converted to the corresponding hitherto unknown 2-aryl-3-iodo-4-(phenylamino)quinoline derivatives using aniline in refluxing ethanol. These 2-aryl-3-iodo-4-(phenylamino)quinolines were reacted with allybromide in ethanol at room temperature to afford 4-(N,N-allylphenylamino)-2-aryl-3-iodoquinoline derivatives. The 2-aryl-3-iodo-4-(phenylamino)quinoline and 4-(N,N-allylphenylamino)-2-aryl-3-iodoquinoline derivatives were subjected to metal-catalysed carbon-carbon bond formations. Palladium(0)-copper iodide catalysed Sonogashira cross-coupling of 2-aryl-3-iodo-4-(phenylamino)quinoline with terminal alkynes afforded series of 1,2,4-trisubstituted 1H-pyrrolo[3,2-c]quinolines in a single step operation. On the other hand, the 4-(N,N-allylphenylamino)-2-aryl-3-iodoquinoline derivatives were found to undergo palladium-catalysed intramolecular Heck reaction to yield the corresponding 1,3,4-trisubstituted 1H-pyrrolo[3,2-c]quinolines. All new compounds were characterized by using a combination of NMR (1H and 13C), IR, mass spectroscopic techniques as well as elemental analysis.

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Lesenyeho, Lehlogonolo Godfrey (2010) Palladium-catalyzed heteroannulation of 2-ARYL- 3-IODO-4-(Phenylamino)quinolines and 4-(N,N-allylphenylamino)-2-ARYL-3-iodoquinolines, University of South Africa, Pretoria, <http://hdl.handle.net/10500/3970>

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