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Efficient synthesis of boron-containing ?-acyloxyamide analogs via microwave irradiation.


ABSTRACT: 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 ?-acyloxyamides under mild conditions within a short time. Two series of boron-containing ?-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.

SUBMITTER: Chai CC 

PROVIDER: S-EPMC6270651 | biostudies-literature | 2013 Aug

REPOSITORIES: biostudies-literature

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Efficient synthesis of boron-containing α-acyloxyamide analogs via microwave irradiation.

Chai Chih-Cheng CC   Liu Pin-Yi PY   Lin Chia-Hung CH   Chen Hsien-Chi HC   Wu Yang-Chang YC   Chang Fang-Rong FR   Pan Po-Shen PS  

Molecules (Basel, Switzerland) 20130808 8


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  ...[more]

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