Three-step synthesis of an array of substituted benzofurans using polymer-supported reagents

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Jörg Habermann, Steven V. Ley and René Smits


Abstract

An efficient combinatorial route to substituted 3-phenylbenzofurans, is achieved by the bromination of acetophenones to α-bromoacetophenones by polymer-supported pyridinium bromide perbromide (PSPBP). The subsequent clean substitution of the obtained bromides by phenols using 1,5,7-triazabicyclo[4.4.0]dec-5-ene (TBD-P) and cyclodehydration of the resulting α-phenoxyacetophenones using Amberlyst 15, affords pure products without the need for any chromatographic purification step.


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