Abstract
Article history: Received January 11, 2012 Received in Revised form Feb 19, 2011 Accepted 2 March 2011 Available online 2 March 2012 A series of novel dihydropyrimidin-2(1H)-ones derivatives was synthesized by using Rhizopus Oryzae lipase biocatalyst in deep eutectic solvent. The reaction is characterized by high efficiency and selectivity, short reaction time, mild and environmentally friendly reaction conditions. The yields were found to be significantly higher and reuse of both the lipase and deep eutectic solvent was possible up to four consecutive cycles. The products are found to exhibit appreciable in vitro antibacterial activity against Echerichia coli, Pseudomonas neumoniae and in vitro antifungal activity against Aspergillus niger and Candida albicans. © 2012 Growing Science Ltd. All rights reserved.
Highlights
Dihydropyrimidin-2(1H)-ones (DHPMs) moieties are common in a variety of biologically important natural products and potent drugs including anti-hypertensive agents, anti-carcinogenic agents, anti-inflammatory, analgesic agents and calcium channel blockers[1,2,3]
The lipase from Rhizopus Oryzae as a biocatalyst is well known in organic synthesis due to its easy availability, selectivity and stability[20]
Earlier we have reported the synthesis of novel styryl colorants[22] and synthesis of trisubstituted alkenes[25] by using lipase as a biocatalyst
Summary
Dihydropyrimidin-2(1H)-ones (DHPMs) moieties are common in a variety of biologically important natural products and potent drugs including anti-hypertensive agents, anti-carcinogenic agents, anti-inflammatory, analgesic agents and calcium channel blockers[1,2,3]. Debache et al.[8] investigated the use of triphenylphosphine as a Lewis base catalyst for the synthesis of DHPMs derivatives It has been reported by using imidazole based ionic liquids (ILs) such as water tolerant Lewis acid [bmim][FeCl4]9, [bmim]BF4 and [bmim]PF610. The lipase from Rhizopus Oryzae as a biocatalyst is well known in organic synthesis due to its easy availability, selectivity and stability[20]. It has found applications in ester hydrolysis[21], knoevenagel condensation[22] and mannich reaction[23], the application in synthesis of DHPMs derivatives has not been well explored. We report for the first time environmentally-benign base catalyzed synthesis of novel DHPMs using lipase biocatalyst in DES and their antimicrobial activity
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