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Synthesis of Tebufenpyrad Analogues using Biotage® Initiator

29 April 2015

Biotage® Initiator microwave synthesizer was used in a study on synthesis of tebufenpyrad analogues to explore potential druglike properties.


A number of fluorinated and fluorine-free pyrazole derivatives were designed and synthesized by a Spanish-US research group to increase understanding of mitochondrial dysfunction, which plays a key role in drug development. The synthetic pathway involves synthesis of 1,3,5-substituted pyrazole precursors, and coupling with key aldehyde intermediates. All microwave reactions were carried out using Biotage microwave reaction vials and Initiator microwave synthesizer. 

The outcome was a range of biologically active fluorinated and fluorine-free analogues of commercial acaricide tebufenpyrad. 

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Raquel Román, Antonio Navarro, Dariusz Wodka, Maria Alvim-Gaston, Saba Husain, Natalie Franklin, Antonio Simón-Fuentes, and Santos Fustero, 2014. Synthesis of Fluorinated and Nonfluorinated Tebufenpyrad Analogues for the Study of Anti-angiogenesis MOA. Org. Process Res. Dev.201418 (8), pp 1027–1036.

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