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Zn(OTf)2-catalyzed cyclization of proparyl alcohols with anilines, phenols, and amides for synthesis of indoles, benzofurans, and oxazoles through different annulation mechanisms
Journal article   Peer reviewed

Zn(OTf)2-catalyzed cyclization of proparyl alcohols with anilines, phenols, and amides for synthesis of indoles, benzofurans, and oxazoles through different annulation mechanisms

Manyam Praveen Kumar and Rai-Shung Liu
Journal of Organic Chemistry, Vol.71(13), pp.4951-4955
23/06/2006

Abstract

Zn(OTf) 2 (10 mol %) catalyzed the cyclization of propargyl alcohols with PhXH (X = O, NH) in hot toluene (100 °C) without additive and gave indole and benzofuran products with different structures. In such transformations, α-carbonyl intermediates A and C were isolated as reaction intermediates. The 1,2-nitrogen shift in the formation of indole is catalyzed by Zn(OTf) 2 , and its mechanism has been elucidated. This catalytic cyclization is also applicable to the synthesis of oxazoles through the cyclization of propargyl alcohols and amides without a 1,2-nitrogen shift. © 2006 American Chemical Society.

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