Regioselective alkylation of 2,4-dihydroxybenzyaldehydes and 2,4-dihydroxyacetophenones

  • Tetrahedron Lett. 2022 Apr 13:95:153755. doi: 10.1016/j.tetlet.2022.153755.
Aziza Frank  1 ,  Negar Hamidi  1 ,  Fengtian Xue  1
Affiliations
  • 1. Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, 20 Penn Street, Baltimore, Maryland 21201, United States.
PMID: 35495552 DOI: 10.1016/j.tetlet.2022.153755
Abstract

We report a cesium bicarbonate-mediated alkylation of 2,4-dihydroxybenzyaldehyde and 2,4-dihydroxyacetophenone to generate 4-alkylated products in acetonitrile at 80 °C with excellent regioselectivity, up to 95% isolated yields, and broad substrate scope.

Keywords
Alkylation; Cesium bicarbonate; Regioselective; Scalable.
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