Synthesis Of Pyrimidine Derivatives Research Articles

Laccase Enzyme Catalyst Mediated Synthesis of Pyrimidines and its Antibacterial, Antifungal, Molecular Docking Studies

The novel synthesis of pyrimidine derivatives (1a-f) by using green chemistry technique with laccase as an enzyme catalyst. FT-IR, 1H NMR, and elemental analyses were used to describe the produced compounds (1a-f). Antibacterial, antifungal, and molecular docking investigations to characterize the produced pyrimidine derivatives (1a-f). In antibacterial testing, compound 1e, showed considerable action towards E. coli (MIC 02 μg/mL) as associated to ciprofloxacin (MIC 04 μg/mL). When related to clotrimazole in antifungal assessment, compound 1d was shown to be significant activity towards C. albicans (MIC 0.25 μg/mL) than clotrimazole (MIC 0.5 μg/mL). Molecular docking experiments further indicate that compound 1e inhibited antibacterial and compound 1d inhibited antifungal proteins more effectively than the control compounds ciprofloxacin and clotrimazole.

An ionic liquids catalyst approach for synthesis of pyrimidine derivatives using l-proline nitrate

An ionic liquids catalyst approach for synthesis of pyrimidine derivatives using l-proline nitrate

Design, synthesis, and herbicidal activity of novel pyrimidine derivatives containing 1,2,4-triazole

A facile approach for the synthesis of pyrimidine derivatives containing 1,2,4-triazole moiety via the reaction of substituted 2-phenoxypropane hydrazide with ethyl-N-(5-cyano-2-alkylthio-5-cyano-6-methylthiopyrimidin-4-yl) formimidate in refluxing 2-methoxyethanol is reported. The structures of the title compounds were identified by 1H NMR, 13C NMR, and HRMS. The configuration of compound 5a was confirmed by X-ray crystallography analysis. The preliminary herbicidal test indicated that some of the target compounds exhibited good inhibition activities against Brassica napus (rape) and Echinochloa crusgalli (barnyard grass).

Ethyl (S)-2-Benzamido-5-[(4,6-dimethylpyrimidin-2-yl)amino]pentanoate

Pyrimidines are compounds with a wide range of biological activities, and the synthesis of pyrimidine derivatives—useful in chemical and medicinal applications—is important in medicinal chemistry. This work shows the synthesis under microwave irradiation of the novel compound ethyl (S)-2-benzamido-5-[(4,6-dimethylpyrimidin-2-yl)amino]pentanoate (3) from (S)-N-α-benzoyl-l-arginine ethyl ester hydrochloride (1) and acetylacetone (2). Compound 3 was easily purified, obtained in moderate yield (70%), and fully characterized by UV-Vis, FTIR-ATR spectroscopy, 1H-NMR, 13C-NMR, HRMS, and EI-MS.

Synthesis of Some New Tetrahydropyrimidine Derivatives as Possible Antibacterial Agents.

Heterocyclic compounds containing a pyrimidine nucleus are of special interests thanks to their applications in medicinal chemistry as they are the basic skeleton of several bioactive compounds such as antifungal, antibacterial, antitumor and antitubercular. As a part of our research in the synthesis of pyrimidine derivatives containing biological activities, some new tetrahydropyrimidine derivatives (1-10) were synthesized via Biginelli reaction using HCl or DABCO as a catalyst with good yields. All structures of products were confirmed by IR, 1H NMR and 13C NMR spectroscopy. The antibacterial activity of some synthesized compounds was investigated against Staphylococcusaureus (ATCC 6538), Staphylococcus epidermidis (ATCC 12228),Bacillus cereus (ATCC14579), Esherichia coli (ATCC 25922), Klebsiella pneumonia (ATCC 13883) and Pseudomonas aeruginosa (PAO1) bacteria. Some of these compounds such as 8 and 10 exhibited a good to significant antibacterial activity.

ChemInform Abstract: A Novel One-Pot Method for the Synthesis of Pyrimidine Derivatives Using Ketene N,S-Acetal with Aryl Aldehydes.

A very simple and facile one-pot method for the synthesis of pyrimidine derivatives is presented. In this method, 2-aryl-pyrimidine derivatives were prepared by the reaction of ketene N,S-acetal 1 with commercially available aryl aldehydes by heating under solvent and catalyst-free conditions. The synthesized pyrimidine derivatives showed blue-green fluorescence in solid state.

ChemInform Abstract: Indium‐Catalyzed Microwave‐Accelerated Pot Economic C—C Bond Formation Process Towards the ′Dry‐Media′ Synthesis of Pyrimidine Derivatives.

An efficient pot and time economic ‘dry-media’ synthesis of pyrimidine core containing scaffolds by application of an indium triflate catalyzed carbon–carbon bond formation procedure through Diels–Alder reaction using microwaves is described. The method is associated with some attractive characteristics such as short reaction time, high yield of products, and recyclability of recovered catalyst from the reaction mixture.

Synthesis and Antimicrobial Activity of some Tetrahydro Quinolone Diones and Pyrano[2,3-d]pyrimidine Derivatives.

There has been special interest in the chemistry of quinolone and pyrimidine derivatives due to their diverse biological activities such as anticonvulsant, anti-malarial agents, antibacterial, antiviral, cytostatic, antithelemintic, antigenotoxic, anti-cancer agents. These compounds are also used as targeting delayed-type hypersensivity and anti-convulsant agents. As a part of our research works in the synthesis of pyrimidine derivatives containing biological activities, a series of novel pyrano[2,3-d]pyrimidine derivatives 2 and tetrahydro quinolone dione derivatives 3 were synthesized via reaction of tetrahydrobenzo[b]pyrano derivatives 1 with different reagents in suitable yields. The characterization of these synthesized compounds was established by IR, (1)H NMR and (13)C NMR spectroscopic data. Furthermore, all compounds were subsequently evaluated for their in-vitro antibacterial activity against three bacteria: Staphylococcus aureus (ATTC-25923), Escherichia Coli (ATTC-25922) and Bacillus anthracic (ATTC-25924).

Indium-catalyzed microwave-accelerated pot economic C–C bond formation process towards the ‘dry-media’ synthesis of pyrimidine derivatives

Substituted pyrimidines can be constructed in good yields via a microwave-accelerated C–C bond formation process through Lewis acid catalysed Diels–Alder reaction from easily available uracil diene and electron deficient acetylene carboxylate.

Synthesis, X-ray diffraction, thermogravimetric and DFT analyses of pyrimidine derivatives.

An eco-benign synthesis of pyrimidine derivatives 2a,b containing different functional groups with different electronic character starting from nitroalkenes 1a and 2b has been described. The structures for 1a and 2a,b have been characterized by single crystal X-ray diffraction analysis. The thermal data of the molecules pointed towards important structural aspects of their stability. The mechanism of their thermal decomposition is discussed. The thermodynamic parameters of the dissociation steps were evaluated and discussed. DFT calculations reveal that the compound 1a possesses a high calculated dipole moment value (8.28 D) which indicates its high reactivity towards its surrounding molecules.

ChemInform Abstract: Synthesis of Pyrimidine Derivatives from Three‐Component Reaction of Malononitrile, Aldehydes and Thiourea/Urea in the Presence of High Surface Area and Nanosized MgO as a Highly Effective Heterogeneous Base Catalyst.

AbstractThe new method is more convenient compared to alternative ways, because it needs shorter reaction times, allows straightforward product isolation, and provides higher yields.

One-Pot and Three-Component synthesis of Substituted Pyrimidines Catalysed by Boron Sulfuric Acid under Solvent-Free Conditions

An efficient, simple and one-pot synthesis of pyrimidine derivatives by a three-component reaction of ketones, triethyl orthoformate, and ammonium acetate in the presence of boron sulfuric acid as a reusable and efficient catalyst under solvent-free conditions is reported. The reusability of catalyst, simplicity of the starting materials, short reaction time, one-pot, and good yields of products are the main advantages.

Synthesis of Pyrimidine Derivatives from Three-component Reaction of Malononitrile, Aldehydes and Thiourea/Urea in the Presence of High Surface Area and Nanosized MgO as a Highly Effective Heterogeneous Base Catalyst

The three-component reaction of malononitrile, aldehydes and thiourea/urea, is applied to the formation of pyrimidine derivatives. The reaction occurs at best in EtOH at reflux, in the presence of high surface area and nanosized MgO. This methodology is more convenient to compare with alternative ways because it needs shorter reaction times, allows straightforward product isolation, and provides higher yields.

Studies on synthesis of pyrimidine derivatives and their antimicrobial activity

A series of novel 2-(5-bromo-2-chloro-pyrimidin-4-ylsulfanyl)-4-methoxy-phenylamine derivatives were synthesized by the reaction of 2-(5-bromo-2-chloro-pyrimidin-4-ylsulfanyl)-4-methoxy-phenylamine with various sulfonyl chlorides, and their in vitro antimicrobial activity was evaluated. The synthesized compounds were characterized by elemental analyses, FT-IR, 1H NMR and LC–MS spectral studies.

ChemInform Abstract: Synthesis of Pyrimidine Derivatives Having Oxo, Thioxo or Amino Functions at Position 4 from 1,2,4-Dithiazolium Salts.

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

ChemInform Abstract: Reaction of Ketene Dithioacetals with Thioamides. A Synthesis of Pyrimidine Derivatives.

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

Novel and Efficient Synthesis of Pyrimidine Derivatives

A new series of 1-alkyl-2-oxo-1,2-dihydro-pyrimidine-5-carboxalic acid amides is described. The reaction of N-((E)-3-(dimethylamino)-2-formylacryloyl) formamidine, an intermediate obtained by Vilsmeier–Haack formylation of acetonitrile with various mono-substituted ureas, provides such compounds in good yields.

Single‐Step Synthesis of Pyrimidine Derivatives.

AbstractChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.

Studies on Synthesis of Pyrimidine Derivatives and their Pharmacological Evaluation

1,3,4‐Oxadiazoles were associated with broad spectrum of biological activities including antituberculosis, anticonvulsant, anti‐inflammatory, insecticidal, antifungal, analgesic and antitumor properties. Morpholine derivatives find their wide spectrum of antimicrobial activity and exhibit anthelmintic, bactericidal and insecticidal activity. Pyrimidine derivatives are also reported to possess antibacterial, antimicrobial, antifungal, anticancer and anticonvulsant activities. Encouraged by this observations we decided to synthesised novel pyrimidine derivatives.

Synthesis, 18F‐Radiolabelling and Biological Evaluations of C‐6 Alkylated Pyrimidine Nucleoside Analogues.

AbstractFor Abstract see ChemInform Abstract in Full Text.