Graphite catalyzed solvent free synthesis of dihydropyrimidin-2(1H)-ones/thiones and their antidiabetic activity |
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| Institution: | 1. Department of Endocrinology, Clinical Medical College, Yangzhou University, Yangzhou 225001, China;2. Institute of Combined Chinese and Western Medicine, Medical College, Yangzhou University, Yangzhou 225001, China;3. Department of Physiology, Nanjing University of Chinese Medicine Hanlin College, Taizhou 225300, China |
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| Abstract: | A solvent free three component condensation reaction between an aldehyde, ethyl acetoacetate and urea catalyzed by graphite, a green catalyst is described for the synthesis of dihydropyrimidin-2(1H)-ones. This protocol is scalable and the catalyst is reusable. This method is also applied for the synthesis of dihydropyrimidin-2(1H)-thiones. α-Amylase, a key enzyme in carbohydrate metabolism is generally targeted for management of type 2 diabetes. The therapeutic potential of the dihydropyrimidinones and dihydropyrimidinthiones to inhibit α-amylase activity was evaluated by in vitro assay. Of the synthesized compounds 3,4-dihydropyrimidin-2(1H)-thione (1k) demonstrated highest inhibition of α-amylase activity. |
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| Keywords: | Biginelli reaction Multicomponent reaction Solvent less Graphite catalysis Dihydropyrimidinones α-Amylase inhibition Antidiabetic |
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