Sonogashira reactions with propyne: Facile synthesis of 4-Hydroxy-2-methylbenzofurans from Iodoresorcinols
The Sonogashira reaction of terminal alkynes and ortho-halophe- nols with subsequent cyclization is a well-precedented method for the synthesis of substituted benzofurans. Here we describe the extension of this method to the coupling of 2-iodoresorcinols and terminal alkynes, including propyne, to give 4-hydroxy-2-substi- tuted benzofurans. In particular, we describe the screening, method development, and scaleup of the reaction with propyne using standard hydrogenation equipment.
Berliner, Martin A.,Cordi, Eric M.,Dunetz, Joshua R.,Price, Kristin E.
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p. 180 - 187
(2010/04/28)
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