4052-92-0Relevant academic research and scientific papers
Aryl uracil compound or agriculturally acceptable salt and preparation method thereof and herbicide composition
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Paragraph 0121; 0125; 0126; 0127; 0128, (2019/02/03)
The invention provides an aryl uracil compound represented by a formula I (shown in the description) or agriculturally acceptable salt thereof. According to the formula I, R1 and R2 are independentlyselected from hydrogen, amino, C1-C4 alkyl or C1-C4 alkyl halide; X and Y are independently selected from hydrogen, halogen, nitryl, cyan, C1-C4 alkyl or substituted C1-C4 alkyl; R3 is selected from hydrogen, cyan or C1-C4 alkyl; and R4 is selected from cyan, nitryl, substituted or unsubstituted phenyl, substituted or unsubstituted five-membered or six-membered aromatic heterocyclic radical or a substituent group represented by a formula II (shown in the description), wherein R5 is selected from halogen, R6 and R7 are independently selected from hydrogen, halogen, C1-C4 alkyl or C1-C4 alkyl halide. The compound has the characteristics of wide weed control spectrum and high herbicidal activity. The invention further provides a preparation method of the aryl uracil compound or the agriculturally acceptable salt of the aryl uracil compound and a herbicide composition.
A New Amphiphilic Br?nsted Acid as Catalyst for the Friedel–Crafts Reactions of Indoles in Water
Cheng, Yuan,Ou, Xiongyu,Ma, Jimei,Sun, Linhao,Ma, Zhong-Hua
, p. 66 - 72 (2019/01/04)
A new amphiphile 1a featuring with two -NHSO2C4F9 sites is designed and synthesized as Br?nsted diacid. The amphiphilicity arose from nano-aggregations of hydrophobic fluorocarbon chains and extension of hydrophilic NH groups, confirmed by Tyndall effect and TEM. The acidity of 1a rivals to concentrated H2SO4, examined by the Hammett acidity function, 31P NMR and conductance titration. Compound 1a demonstrated excellent catalytic performance in the Friedel–Crafts alkylation of indoles in water. Reactive substrates, such as β-monosubstituted vinyl ketones in 1,4-addition and aldehydes in condensation, were quantitatively converted, and the products were easily isolated by filtration or extraction in 85–96 % yields. Additionally, there was no observation of effect of the acidity weakening of 1a on catalysis when poor-reactive substrates were used, such as β,β-disubstituted vinyl ketones in 1,4-addition and ketones in condensation. The two kinds of reactions were practised very smoothly. The formed nano-aggregations and the strong acidity of 1a were responsible for the highly efficient aqueous catalysis. Notably, 1a was recycled at least 3 times thanks to its amphiphilic structure. It was demonstrated the nano-aggregations played a key role in the aqueous synthesis.
METHOD FOR PRODUCING DICARBOXYLIC ACID COMPOUND
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Paragraph 0177; 0180, (2018/06/09)
It is an object of the present invention to provide an excellent method for producing an excellent therapeutic agent. The solution of the present invention is as shown in the following scheme: wherein R1 represents a C1-C6 alkyl group, R2 represents a C1-C6 alkyl group, and R3 represents a C1-C6 alkyl group.
Method for preparing 3-chlorosulfonylbenzoyl chloride
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Paragraph 0033; 0034; 0035, (2018/09/08)
The invention discloses a method for preparing 3-chlorosulfonylbenzoyl chloride. The method comprises the following steps: (1) benzoic acid and excess chlorosulfonic acid are subjected to a sulfonylation reaction with 20 wt% fuming sulfuric acid as a catalyst to prepare a sulfonating liquid; and (2) the sulfonating liquid prepared in the step (1) and oxalyl chloride are subjected to an acylation reaction with DMF as a catalyst to prepare the target product 3-chlorosulfonylbenzoyl chloride. The method has mild reaction conditions, short reaction time, simple operation, high yield, good productquality, and almost no pollution to environment, is suitable for industrial production, and has a very good application prospect.
Nitrogen-containing heterocycle derivatives and applications thereof
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Paragraph 0223-0225, (2018/03/24)
The invention discloses nitrogen-containing heterocycle derivatives and applications thereof, relates to compounds of a general formula (V), a preparing method thereof and applications of the compounds in medicines, and more particularly relates to compound derivatives of compounds shown as the general formula (V), a preparing method thereof and uses of the derivatives in medicines preventing andtreating hyperlipemia, hypercholesterolemia, hypertriglyceridemia, fatty degeneration of liver, diabetes mellitus type 2, hyperglycemia, obesity or insulin resistance and metabolic syndrome and resisting antitumor, with the derivatives being adopted as therapeutic agents. The compounds disclosed by the invention can also reduce total cholesterol, LDL-cholesterol and triglyceride, can increase liver LDL receptor expression, and inhibit PCSK9 expression.
A chemoselective and continuous synthesis of m-sulfamoylbenzamide analogues
Verlee, Arno,Heugebaert, Thomas,Van Der Meer, Tom,Kerchev, Pavel I.,Van Breusegem, Frank,Stevens, Christian V.
supporting information, p. 303 - 312 (2017/03/14)
For the synthesis of m-sulfamoylbenzamide analogues, small molecules which are known for their bioactivity, a chemoselective procedure has been developed starting from m-(chlorosulfonyl)benzoyl chloride. Although a chemoselective process in batch was already reported, a continuous-flow process reveals an increased selectivity at higher temperatures and without catalysts. In total, 15 analogues were synthesized, using similar conditions, with yields ranging between 65 and 99%. This is the first automated and chemoselective synthesis of m-sulfamoylbenzamide analogues.
Identification and Optimization of Anthranilic Acid Based Inhibitors of Replication Protein A
Patrone, James D.,Pelz, Nicholas F.,Bates, Brittney S.,Souza-Fagundes, Elaine M.,Vangamudi, Bhavatarini,Camper, Demarco V.,Kuznetsov, Alexey G.,Browning, Carrie F.,Feldkamp, Michael D.,Frank, Andreas O.,Gilston, Benjamin A.,Olejniczak, Edward T.,Rossanese, Olivia W.,Waterson, Alex G.,Chazin, Walter J.,Fesik, Stephen W.
supporting information, p. 893 - 899 (2016/05/09)
Replication protein A (RPA) is an essential single-stranded DNA (ssDNA)-binding protein that initiates the DNA damage response pathway through protein-protein interactions (PPIs) mediated by its 70N domain. The identification and use of chemical probes that can specifically disrupt these interactions is important for validating RPA as a cancer target. A high-throughput screen (HTS) to identify new chemical entities was conducted, and 90 hit compounds were identified. From these initial hits, an anthranilic acid based series was optimized by using a structure-guided iterative medicinal chemistry approach to yield a cell-penetrant compound that binds to RPA70N with an affinity of 812 nm. This compound, 2-(3- (N-(3,4-dichlorophenyl)sulfamoyl)-4-methylbenzamido)benzoic acid (20 c), is capable of inhibiting PPIs mediated by this domain.
Fluorescent non-peptidic RGD mimetics with high selectivity for αvβ3 vs αiIbβ3 integrin receptor: Novel probes for in vivo optical imaging
Alsibai, Wael,Hahnenkamp, Anke,Eisenbl?tter, Michel,Riemann, Burkhard,Sch?fers, Michael,Bremer, Christoph,Haufe, Günter,H?ltke, Carsten
, p. 9971 - 9982 (2015/02/02)
Integrins are heterodimeric transmembrane protein receptors consisting of different α and β subunits. αvβ3 integrins are overexpressed on many tumor cells and tumor-associated angiogenic vessels, whereas αIIbβ3 is a receptor for, e.g., fibrinogen and mediates platelet aggregation. In this study, a near-infrared fluorescent imaging probe has been designed and synthesized by conjugating fluorescent dyes to a non-peptidic, pharmacophore-based ligand, based on a molecular modeling design approach. Affinity values were determined, and in vitro cell binding assays and preliminary in vivo xenograft studies in nude mice were performed to evaluate target binding. Competition assays revealed excellent binding and selectivity to αvβ3 compared to that for αIIbβ3. In vitro, the probe showed high target binding on αvβ3-positive M-21 cells and negligible binding to αvβ3-negative MCF-7 cells. In vivo, the tracer is able to image target expression in U-87 xenografts with a maximum signal-to-noise ratio (SNR) of 2.5:1 at 24 h after injection.
HEPATITIS B ANTIVIRAL AGENTS
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Page/Page column 233, (2013/07/05)
The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.
Phosphopeptide-dependent labeling of 14 - 3 - 3 ζ proteins by fusicoccin-based fluorescent probes
Takahashi, Michiko,Kawamura, Akie,Kato, Nobuo,Nishi, Tsuyoshi,Hamachi, Itaru,Ohkanda, Junko
supporting information; experimental part, p. 509 - 512 (2012/03/11)
Fluorescent combination: Cell-penetrating probes derived from the diterpene fusicoccin can form ternary complexes with 14-3-3 proteins and phosphopeptide ligands, whereupon the probes site-specifically attach a fluorescent tag onto the surface of the 14-3-3 proteins. Copyright
