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

Journal of the Brazilian Chemical Society

Amaral, Mônica F. Z. J.¹  Toledo, Fabiano T.¹  Clososki, Giuliano C.¹  Universidade de São Paulo, Ribeirão Preto, Brazil¹  Callejon, Daniel R.¹  Riul, Thalita B.¹  Lopes, Norberto P.¹  Baruffi, Marcelo D.¹  Lychnoflora Pesquisa e Desenvolvimento em Produtos Naturais LTDA, Ribeirão Preto, Brazil¹ 

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

DOI  :  10.5935/0103-5053.20140196

学科分类：化学（综合）

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】

Unknown