201287-93-6Relevant academic research and scientific papers
Structure-based designing, solvent less synthesis of 1,2,3,4-tetrahydropyrimidine-5-carboxylate derivatives: A combined in vitro and in silico screening approach
Ahmad, Zaheer,Ahmed, Sibtain,Akhtar, Naseem,Arshad, Uzma,Hassan, Aqsa,Mehmood, Tahir,Parveen, Shagufta,Shafiq, Nusrat
, (2021)
Objective: In this study, small molecules possessing tetrahydropyrimidine derivatives have been synthesized having halogenated benzyl derivatives and carboxylate linkage. As previously reported, FDA approved halogenated pyrimidine derivatives prompted us
Synthesis method of dihydropyrimidinone compound
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Paragraph 0034-0036; 0040-0041; 0044; 0070-0075; 0078, (2021/05/19)
The invention discloses a synthesis method of a dihydropyrimidone compound, which belongs to the technical field of organic synthesis, and comprises the following steps: by taking benzaldehyde or a derivative thereof, ethyl acetoacetate or acetylacetone a
Preparation method of 3,4-dihydropyrimidine-2(1H)-one compound
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Paragraph 0021-0022; 0030-0032, (2020/09/30)
The invention discloses a preparation method of a 3,4-dihydropyrimidine-2(1H)-one compound, wherein the comprises the steps: (1) respectively adding reaction substrate raw materials aromatic aldehydes, 1,3-diketone ester, urea and a trace amount of water
One pot synthesis of micromolar BACE-1 inhibitors based on the Dihydropyrimidinone scaffold and their Thia and Imino analogues
Bais, Jessica,Benedetti, Fabio,Berti, Federico,Cerminara, Iole,Drioli, Sara,Felluga, Fulvia,Funicello, Maria,Regini, Giorgia,Vidali, Mattia
, (2020/09/18)
A library of dihydropyrimidinones was synthesized via a “one-pot” three component Biginelli reaction using different aldehydes in combination with β-dicarbonyl compounds and urea. Selected 2-thiooxo and 2-imino analogs were also obtained with the Biginell
Metal- And Oxidant-Free Electrochemical Oxidative Desulfurization C-O Coupling of Thiourea-Type Compounds with Alcohols
Cao, Bao-Qian,Quan, Zheng-Jun,Ren, Ming-Zhe,Wang, Xi-Cun,Zhu, Zheng-He
supporting information, p. 1634 - 1642 (2020/05/25)
An efficient desulfurization C-O coupling reaction of 3,4-dihydropyrimidine-2(1 H)-thiones (including thioureas) with alcohols was developed under electrochemical oxidation conditions. Herein, transition--metal catalysts and additives are not required and
Ionic liquid-assisted synthesis of dihydropyrimidin(thi)one Biginelli adducts and investigation of their mechanism of urease inhibition
Braga, Taniris Cafiero,Silva, Thamara Ferreira,MacIel, Thamilla Maria Silva,Da Silva, Edjan Carlos Dantas,Da Silva-Júnior, Edeildo Ferreira,Modolo, Luzia Valentina,Figueiredo, Isis Martins,Santos, Josué Carinhanha Caldas,De Aquino, Thiago Mendon?a,De Fátima, ?ngelo
, p. 15187 - 15200 (2019/10/08)
Twenty-six Biginelli adducts were synthesized through an ionic liquid-assisted synthesis with up to 92% yield. Sixteen of these Biginelli adducts were then assayed to determine their antiureolytic activity against purified urease from jack beans. The substances BA7-S, BA9-S and BA11-S were shown to be as efficient inhibitors as hydroxyurea, a positive control used in in vitro screening assay against urease. Fluorescence studies revealed that BA7-S, BA9-S, BA11-S and BA5-S possessed high binding constant values of 5.95, 6.72, 4.55, and 4.28 M-1, respectively, while BAS12-S, without substituents, showed a low value of log Kb = 2.16 M-1. In addition, in the most thermodynamically favorable BA5-S and BA7-S urease complexes, the corresponding Biginelli adducts were capable of interacting with the active site of urease through non-ionic interactions, such as hydrophobic interactions, or hydrogen and van der Waals interactions, respectively. In silico studies also supported that the BAs interact with the active site, confirming the fluorescence and kinetic assay studies, which clearly indicate that BA5-S and BA7-S are competitive inhibitors (Ki = 0.96 and 0.57 mM, respectively). In silico studies also showed that the substituents in the aromatic ring interact with Ni atoms to form a stable complex.
UV-Light-Irradiated Trifluoromethylation of Diheteroaryl Disulfides with CF3SO2Na
Cao, Bao-Qian,Qiu, Yi-Feng,Zhang, Xi,Zhu, Zheng-He,Quan, Zheng-Jun,Wang, Xi-Cun
supporting information, p. 1208 - 1214 (2019/02/07)
A simple protocol for the UV light irradiated preparation of heteroaryl trifluoromethyl thioethers from disulfides and inexpensive, environmentally sodium triflinate (CF3SO2Na) has been developed. The features of simple and clean rea
Br?nsted acidic 1-ethyl-1,2,4-trizolium phenylsulfonate as catalyst for biginelli reaction
Puthukkudy,Nagarajan,Kandasamy
, p. 1999 - 2002 (2018/08/09)
A Br?nsted acidic 1-ethyl-1,2,4-triazolium phenylsulfonate has been synthesized and characterized. A catalytic study is performed for 1-ethyl-1,2,4-triazolium phenylsulfonate as acid catalyst for a multicomponent reaction of synthesis of series of 3,4-dih
T3P-DMSO mediated one-pot tandem approach for the synthesis of 3,4-Dihydropyrimidin-2(1H)-ones/thiones from alcohols
Vinaya, Kambappa,Shivaramu, Prasanna D.,Chandrashekara, Ganganahalli K.,Chandrappa, Siddappa,Rangappa, Kanchugarakoppal S.
, p. 241 - 245 (2018/04/20)
Background: Biginelli reaction is one of the most important multiple-component chemical reactions which creates 3,4-dihydropyrimidin-2(1H)-ones. Even though Biginelli reaction was reported over a century using different substrates, literature lacks the ex
Punica granatum peel: an organocatalyst for green and rapid synthesis of 3,4-dihydropyrimidin-2 (1H)-ones/thiones under solvent-free condition
Mohammadian, Narges,Akhlaghinia, Batool
, p. 3325 - 3347 (2017/04/21)
A novel and green approach was adopted for the synthesis of 3,4-dihydropyrimidin-2(1H)-one/thiones derivatives using Punica granatum peel as an inexpensive, efficient and mild catalyst under solvent-free condition. The methodology is characterized by high
