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Preferred term

Biginelli reaction  

Definition

  • The Biginelli reaction is a multiple-component chemical reaction that creates 3,4-dihydropyrimidin-2(1H)-ones 4 from ethyl acetoacetate 1, an aryl aldehyde (such as benzaldehyde 2), and urea 3. It is named for the Italian chemist Pietro Biginelli. This reaction was developed by Pietro Biginelli in 1891. The reaction can be catalyzed by Brà¸nsted acids and/or by Lewis acids such as copper(II) trifluoroacetate hydrate and boron trifluoride. Several solid-phase protocols utilizing different linker combinations have been published. Dihydropyrimidinones, the products of the Biginelli reaction, are widely used in the pharmaceutical industry as calcium channel blockers, antihypertensive agents, and alpha-1-a-antagonists. More recently products of the Biginelli reaction have been investigated as potential selective Adenosine A2b receptor antagonists. Including highly selective tricyclic compounds.

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http://data.loterre.fr/ark:/67375/37T-R971T6K5-V

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