- Thiazolidin-4-one formation. Mechanistic and synthetic aspects of the reaction of imines and mercaptoacetic acid under microwave and conventional heating
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Microwave irradiation of a mixture of benzylidene-anilines and mercaptoacetic acid in benzene gives 1,3-thiazolidin-4-ones in very high yield (65-90%), whereas the same reaction performed through using the conventional method, at reflux temperature, requires a much longer time and gives a much lower yield (25-69%). This difference seems to be due to some intermediates and by-products formed during the conventional reaction. On the basis of 1H NMR studies, two different mechanisms, acting in benzene and in DMF, respectively, have been hypothesized for the thiazolidin-4-one system formation.
- Bolognese, Adele,Correale, Gaetano,Manfra, Michele,Lavecchia, Antonio,Novellino, Ettore,Barone, Vincenzo
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p. 2809 - 2813
(2007/10/03)
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- Synthesis and Anihistaminic Activity of Some Thiazolidin-4-ones
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A new series of 2-(4- and 3-substituted phenyl)-3--1,3-thiazolidin-4-ones were synthesized, characterized, and evaluated for their ability to inhibit the contractions induced by histamine on guinea pig ileum.The measurement of pA2 values suggested that the reported compounds showed H1-antagonism.The more active compounds 5,9 and 13 exhibited activity close to that of mepyramine.
- Diurno, M. Vittoria,Mazzoni, Orazio,Piscopo, Eugenio,Calignano, Antonio,Giordano, Federico,Bolognese, Adele
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p. 2910 - 2912
(2007/10/02)
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