Antimony(III) chloride-catalysed Biginelli reaction: a versatile method for the synthesis of dihydropyrimidinones through a different reaction mechanism |
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Authors: | Ivica Cepanec,Mladen Litvi?,Mirela Filipan-Litvi?,Ivana Grü ngold |
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Affiliation: | BELUPO Pharmaceuticals Inc., Research Department, Radni?ka c. 224, 10000 Zagreb, Croatia |
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Abstract: | Antimony(III) chloride (20 mol %) in refluxing acetonitrile efficiently catalyses the synthesis of dihydropyrimidinones (50-90% yields) by the Biginelli reaction of aromatic aldehydes, acetoacetate esters and urea. This reaction proceeds through 3-ureido-crotonates followed by cyclisation with an aromatic aldehyde to the dihydropyrimidinone. |
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