Application of the Negishi reaction in the synthesis of thiophene-based lignans analogues with leishmanicidal effects

Journal of the Brazilian Chemical Society

Mônica F. Z. J. Amaral²  Daniel R. Callejon²  Thalita B. Riul¹  Marcelo D. Baruffi¹  Fabiano T. Toledo²  Norberto P. Lopes²  Giuliano C. Clososki² 

[1] ,Universidade de São Paulo Faculdade de Ciências Farmacêuticas de Ribeirão Preto Ribeirão Preto SP ,Brazil

关键词: thiophene;    leishmanicidal;    Negishi reaction;    cross-coupling;    green chemistry;   

DOI  :  10.5935/0103-5053.20140196

来源: SciELO

【 摘 要 】

Lignans represent a well-known group of natural products with anti-protozoal activity. In the literature there are many examples of the anti-parasitic activity of synthetic analogues of lignans containing sulphur bridges. In this work, we have obtained thiophene-based analogues by using a selective and high performance synthetic strategy based on the Negishi cross-coupling reaction. The derivatives were quickly obtained and showed great purity, low toxicity toward a mammalian cell line, and leishmanicidal activity with different potencies.

【 授权许可】

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