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Biological and Pharmaceutical Bulletin
Vol. 39 (2016) No. 2 p. 267-271

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http://doi.org/10.1248/bpb.b15-00681

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In this work, the catalytic activity of calix[8]arene sulfonic acid was successfully investigated for the famous Biginelli reaction. Under ultrasonic irradiation, calix[8]arene sulfonic acid could efficiently catalyzed the three-component reaction of aldehydes with ethyl acetoacetate and urea or thiourea in ethanol to afford the corresponding 3,4-dihydropyrimidin-2(1H)-ones/thiones in 46–93%. The advantages of this method are the easy isolated procedure, short reaction time and low cost of the catalyst.
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