Synthesis, characterization and antifungal testing of 3,4-dihydropyrimidin-2(1H)-(thio)ones containing boronic acids and boronate esters

• DOI: 10.2478/s11532-008-0064-x
• Publication Date: 2008-10-27T21:26:44Z
• Authors: Dominique Duguay; Matthew Zamora; Johanna Blacquiere; Francis Appoh; Christopher Vogels; Susan Wheaton; Felix Baerlocher; Andreas Decken; Stephen Westcott
• Keywords: 01 natural sciences; 3. Good health; 0104 chemical sciences

Abstract The addition of formylphenylboronic acid derivatives to thiourea and ethyl acetoacetate proceeds in the presence of an additional Lewis acid catalyst to give the corresponding 3,4-dihydropyrimidin-2(1H)-(thio)ones (Biginelli products) in moderate yield. Compounds were tested for antifungal activity against pure cultures of Aspergillus niger, Aspergillus flavus, Candida albicans and Saccharomyces cerevisiae but, unfortunately, none showed any appreciable activity.