Refernces
10.1016/j.ejmech.2010.01.032
The study focuses on the synthesis and evaluation of a series of new acrylamide derivatives containing 1,2,3-thiadiazole for their potential antiviral activity against hepatitis B virus (HBV) replication. These compounds were designed based on the structure of known anti-HBV agents and synthesized through various chemical reactions. The in vitro anti-HBV activities were assessed by measuring the inhibition of HBV DNA replication, secretion of HBeAg, and HBsAg in 2.2.15 cells. The results showed that several compounds, particularly 9c, demonstrated higher inhibitory activity against HBV DNA replication compared to the positive control lamivudine. Additionally, compound 9d exhibited significant activity against the secretion of HBeAg. The study concludes that these acrylamide derivatives containing 1,2,3-thiadiazole could serve as promising candidates for the development of new anti-HBV drugs.
10.1080/00397910802419680
The research focuses on the efficient synthesis of 7-amino-3-hydroxyindan-1-one, a three-dimensional, three-point scaffold with potential applications in constructing focused compound libraries for biological interactions. The synthesis is achieved through a three-step process: first, reacting 4-nitrophthalic anhydride with ethyl acetoacetate, acetic anhydride, and triethylamine in methylene chloride to produce compound 10; second, hydrolyzing and decarboxylating compound 10 with trifluoroacetic acid in acetonitrile to yield 4-nitroindan-1,3-dione (11); and third, reducing compound 11 using catalytic hydrogenation with 10% Pd/C in methanol to obtain the final product, 7-amino-3-hydroxyindan-1-one (7). The structure of compound 7 was confirmed using heteronuclear multiple bond correlation (HMBC) spectral studies. The article also details the preparation of N-substituted derivatives of compound 7 and provides their physical constants, spectral data, and yields. Analytical techniques used include NMR spectroscopy, LC/MS, and melting point determination, ensuring the purity and structure of the synthesized compounds.
10.1021/op300162d
The research focuses on the optimization of the reductive debenzylation of hexabenzylhexaazaisowurtzitane (HBIW), a key step in the synthesis of high energy density material HNIW (CL-20). The study employs palladium hydroxide on activated carbon as a catalyst, characterized using techniques like nitrogen adsorption/desorption isotherm, hydrogen isotherm, SEM, and TEM. A central composite design (CCD) was utilized to optimize reaction conditions, examining the impact of four variables: catalyst to HBIW percent, reaction temperature, hydrogen pressure, and acetic anhydride (Ac2O) mole ratio on reaction yield. The optimal conditions were determined to be 20% (w/w) catalyst to HBIW, 48.5°C reaction temperature, 4.25 bar hydrogen pressure, and an Ac2O/HBIW mole ratio of 10.9, resulting in a 73% yield. The experiments involved the use of HBIW, DMF, acetic anhydride, and bromobenzene, with the synthesized product TADB characterized by melting point and TLC. The catalyst was analyzed for surface area, pore size distribution, active surface area, and palladium distribution using the aforementioned techniques.
10.1080/00304940809458105
The research focuses on an improved, Lewis acid-free approach for the synthesis of protected racemic cyanohydrins, which are valuable in pharmaceuticals and agrochemicals. The study utilizes a three-component reaction involving benzaldehyde, sodium cyanide, and acetic anhydride in an eco-friendly solvent, PEG-400, at room temperature. This method yields protected racemic cyanohydrins with moderate to excellent results, comparable to Lewis acid-catalyzed reactions. The experiments conducted encompass a series of sterically and electronically differentiated aromatic substrates, as well as aliphatic and heteroaromatic aldehydes, to define the scope of the synthesis. The analyses used to characterize the products include 'H NMR, 13C NMR, IR spectroscopy, mass spectrometry, and elemental analysis, providing comprehensive data on the structure and composition of the synthesized cyanohydrins.
10.1080/00397910008086885
The research details a versatile approach to synthesizing protected (S)-aspartimide, (4S)-amino-2-pyrrolidinone, and (3S)-aminopyrrolidine derivatives starting from (S)-aspartic acid. The purpose of this study was to develop a unified method for these structurally related compounds, which are significant due to their presence in various bioactive compounds and their potential use as chiral ligands in asymmetric synthesis. The researchers successfully synthesized (S)-1-benzyl-3-p-toluenesulfonylamino-2,5-pyrrolidinedione, (S)-1-benzyl-3-p-toluenesulfonylaminopyrrolidine, and (S)-1-benzyl-4-p-toluenesulfonylamino-2-pyrrolidinone using a series of reactions involving tosylation, cyclization, and selective reductions. Key chemicals used in the process included (S)-aspartic acid, acetic anhydride, benzylamine, lithium aluminium hydride, sodium borohydride, and various solvents such as ethyl acetate and tetrahydrofuran (THF). The study concluded with the establishment of a useful approach to these compounds, which are valuable building blocks for several bioactive compounds, and noted that further investigation into the use of the synthesized compounds as chiral ligands for asymmetric synthesis is underway.
10.1016/S0040-4039(97)01204-5
The research focuses on the one-pot synthesis of 1-allyl- and 1-allenyl-6-O-acetyl-2,3,4-tri-O-benzyl-α-D-glycosides from methyl tetra-O-benzyl-α-D-glycosides. The purpose of this study was to develop an efficient method for the synthesis of these glycosides, which are potential drug candidates for the treatment of inflammatory diseases, and are superior to the parent carbohydrates. The researchers achieved this by using allyl trimethylsilane or propargyl trimethylsilane in the presence of trimethylsilyl trifluoromethanesulfonate (TMSOTf), followed by the addition of acetic anhydride. The process was found to be quite general and effective, yielding the desired products in good yields. The chemicals used in this process include methyl per-benzyl-α-D-glycosides, allyl trimethylsilane, propargyl trimethylsilane, TMSOTf, and acetic anhydride. The conclusions of the study highlight the ease and effectiveness of the new method for synthesizing 6-acetyl-C-linked glycosides, which are useful building blocks for the synthesis of various C-glycosides with modification at the C-6 position.
10.1016/S0040-4039(00)85245-4
The study explores the synthesis of acetoxy-2 bromo-3 propene-2 nitriles using gem-dicyanoepoxides. The key chemicals involved include gem-dicyanoepoxides, which serve as the starting materials for the nucleophilic ring-opening reactions. The complex Li2NiBr4 plays a crucial role as a nucleophile, facilitating the ring-opening process to form new capto dative compounds. Acetic anhydride is used to acetylate the intermediate products, leading to the formation of the desired acetoxy-2 bromo-3 propene-2 nitriles. The study highlights the reactivity of these compounds, which can be considered as equivalents of carbenes with inverted polarity. They can undergo cycloaddition reactions with Diels-Alder adducts and react with carbenes to form cyclopropanes. The synthesized compounds are characterized by various spectroscopic techniques, including IR, NMR, and mass spectrometry, confirming their structures and providing insights into their potential applications in heterocyclic chemistry.
10.1016/j.cclet.2010.03.016
The study focuses on the design, synthesis, and in vitro cytotoxicity evaluation of a series of quinoline-3-carbonitrile derivatives against four cancer cell lines: A549 (lung), HT-29 (colon), MDA-MB-231 (breast), and SMMC-7721 (liver). The research aimed to develop potent and selective anti-tumor agents by replacing the quinazoline scaffold of Gefitinib, an EGFR tyrosine kinase inhibitor, with a quinoline-3-carbonitrile scaffold. The synthesized compounds were tested for their cytotoxic effects using the MTT assay, and the results showed that several of these derivatives exhibited superior selective cytotoxicity against the SMMC-7721 cell line compared to Gefitinib, with compound 11g being the most potent among them. The study also provided preliminary insights into the structure-activity relationships of these compounds, suggesting their potential as anti-cancer agents. Further research on their anti-tumor activities and detailed structure-activity relationships is ongoing.
10.1021/jo00331a016
The study presents a chemical method for converting folic acid to pteroic acid, a valuable intermediate for synthesizing folic acid analogues and derivatives. The process involves treating folic acid with acetic anhydride to form a mixture of acetylated azlactones, which are then cleaved with mild base to yield mainly acetylated pteroic acids. Further treatment with hot base removes the acetyl groups, resulting in pteroic acid with a yield of 55-60% contaminated with folic acid. The study also discusses various side reactions and byproducts, including the formation of a pyrazine derivative from the hydrolysis of the glutamic acid moiety and the opening of the pyrimidine ring. The authors detail the experimental procedures, including HPLC analysis, UV absorption spectra, mass spectrometry, and proton NMR spectra, and provide a method for separating folic and pteroic acids using column chromatography. The research was supported by a grant from the National Cancer Institute, National Institutes of Health.
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C
C:Corrosive;
