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

Molecules

Chih-Cheng Chai²  Pin-Yi Liu²  Chia-Hung Lin²  Hsien-Chi Chen²  Yang-Chang Wu¹  Fang-Rong Chang³ 

[1] School of Pharmacy, College of Pharmacy, China Medical University, Taichung 404, Taiwan;Department of Chemistry, Tamkang University, New Taipei 25137, Taiwan;Graduate Institute of Natural Products, Kaohsiung Medical University, Kaohsiung 807, Taiwan

关键词: boron;    multicomponent reaction;    Passerini reaction;    HepG2;   

DOI  :  10.3390/molecules18089488

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2013 by the authors; licensee MDPI, Basel, Switzerland.