Molecules (Aug 2013)

Efficient Synthesis of Boron-Containing α-Acyloxyamide Analogs via Microwave Irradiation

  • Po-Shen Pan,
  • Fang-Rong Chang,
  • Chia-Hung Lin,
  • Hsien-Chi Chen,
  • Yang-Chang Wu,
  • Pin-Yi Liu,
  • Chih-Cheng Chai

DOI
https://doi.org/10.3390/molecules18089488
Journal volume & issue
Vol. 18, no. 8
pp. 9488 – 9511

Abstract

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In this report, a Passerini three-component reaction utilizing boron-containing carboxylic acids or aldehydes is discussed. The reaction was carried out in water and facilitated by the use of microwave irradiation. This methodology allowed for the efficient formation of a broad range of boron-containing α-acyloxyamides under mild conditions within a short time. Two series of boron-containing α-acyloxyamides were synthesized and subsequently screened for cytotoxicity using the MTT cell viability assay. Two potential lead compounds were found to have potent activity against the HepG2 cancer cell line, demonstrating the potential of this methodology for use in the development of novel pharmaceuticals.

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