- A mild and practical method for the regioselective synthesis of N-acylated 3,4-dihydropyrimidin-2-ones. New acyl transfer reagents
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The treatment of 3,4-dihydropyrimidin-2-ones with n-BuLi at -78 °C, followed by quenching with various electrophiles furnished N3-substituted derivatives, regioselectively. Further, N1,N3-diacyl derivatives were found to transfer N1-acyl groups to nucleop
- Singh, Kamaljit,Singh, Sukhdeep
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- A domino desulfitative coupling/acylation/hydration process cocatalyzed by copper(I) and palladium(II): Synthesis of highly substituted and functionalized pyrimidines
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A domino desulfitative coupling/acylation/hydration process to synthesize C-2-(2-oxo-2-phenylethylidene)- and N-3-carbonyl-substituted pyrimidines by unprecedented C-C and C-N cross-coupling reactions is described. This methodology couples 3,4-dihydropyrimidine-2-thiones and alkynes under modified Liebeskind-Srogl conditions using palladium acetate and copper(I) carboxylate. Remarkably the copper(I) carboxylates simultaneously act as desulfitative and acylation reagents in the reaction. Copyright
- Quan, Zheng-Jun,Hu, Wang-Hua,Jia, Xiao-Dong,Zhang, Zhang,Da, Yu-Xia,Wang, Xi-Cun
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supporting information
p. 2939 - 2948
(2013/01/15)
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- Efficient and convenient synthesis of N3-(acyloxymethyl) dihydropyrimidinones by a one-pot two-step method
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3,4-Dihydropyrimidinones modified with N3-(acetoxymethyl) and (aroyloxymethyl) groups can be regioselectively obtained in good yields by reactions of 3,4-dihydropyrimidinones with paraformaldehyde and substituted benzoic acids/acetic acid, by a one-pot two-step strategy in the presence of chlorotrimethylsilane. The advantages of this method are the simple procedure, the high regioselectivity of the products, shorter reaction time and the mild reaction conditions. Additionally, this method directly uses acid as acylation reagents and needs not acid anhydride or acyl chloride.
- Quan, Zheng-Jun,Ren, Rong-Guo,Da, Yu-Xia,Zhang, Zhang,Wang, Xi-Cun
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p. 188 - 192
(2012/04/04)
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- N1,N3-Diacyl-3,4-dihydropyrimidin-2(1H)-ones: neutral acyl group transfer reagents
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Readily available N1,N3-diacyl-3,4-dihydropyrimidin-2(1H)-ones efficiently acylate ammonia, primary and secondary amines to furnish primary, secondary and tertiary amides in good to excellent yields. The wide applicability of the procedure is demonstrated
- Singh, Kamaljit,Singh, Kawaljit
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experimental part
p. 10395 - 10399
(2010/02/28)
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- QSAR analysis of 2-oxo-1,2,3,4-tetrahydropyrimidine analogues of antibacterials
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QSAR analysis of two sets of analogues of 2-oxo-1,2,3,4- tetrahydropyrimidine was performed to investigate the relationship between their physicochemical parameters and antibacterial activity. Predictive and statistically significant models were generated
- Sawant, Ramesh L.,Bhatia, Manish S.
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experimental part
p. 1361 - 1373
(2010/04/28)
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- High-throughput synthesis of N3-acylated dihydropyrimidines combining microwave-assisted synthesis and scavenging techniques
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(Matrix presented) The solution-phase synthesis of N3-acylated dihydropyrimidines was achieved utilizing microwave flash heating both in the synthesis (acylation) and purification (scavenging) steps. Quenching times for excess anhydrides using polystyrene
- Dallinger, Doris,Gorobets, Nikolay Yu.,Kappe, C. Oliver
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p. 1205 - 1208
(2007/10/03)
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