2459-05-4Relevant articles and documents
Kras-G12C inhibitor heterocyclic compounds
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Paragraph 0239; 0242-0245, (2021/06/23)
The invention relates to Kras-G12C inhibitor heterocyclic compounds represented by formula I, a preparation method thereof, and application of the Kras-G12C inhibitor heterocyclic compounds in prevention and treatment of tumor diseases such as lung cancer, colorectal cancer and pancreatic cancer. In the preparation process, the compounds of the general formula I are obtained through a series of reactions such as SN2 reaction, protection, coupling reaction, deprotection, condensation reaction and the like.
Application of fumaric acid monoethyl ester silver salt in preventing novel coronavirus infections
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Paragraph 0022, (2020/06/09)
The invention discloses application of fumaric acid monoethyl ester silver salt in preventing novel coronavirus infections. The application comprises the following steps: adding 1000g of fumaric acidmonoethyl ester into a reaction bottle of 5L, adding 3Kg of pure water, adding 100g of nano silver oxide while stirring, performing a stirring reaction for 9 hours, filtering the reaction liquid to remove impurities, performing vacuum distillation to spin off moisture at 60 DEG C, adding 5Kg of ethanol, performing stirring crystallization for 4.5 hours, performing filtering, collecting a solid, and performing vacuum drying on the obtained solid for 6 hours at 75 DEG C, so as to obtain the fumaric acid monoethyl ester silver salt. The fumaric acid monoethyl ester silver salt is applied to treatment and prevention on various coronaviruses. Experiments show that with a concentration of 500[mu] g/mL, a fumaric acid monoethyl ester silver salt dissolved solution has an inhibition rate of 99.9%upon coronavirus main protease, a corresponding zinc salt dissolved solution and a silver salt dissolved solution of the fumaric acid monoethyl ester silver salt have inhibition rates of 99.9% and 99.7% upon the coronavirus main protease respectively, and the effects are remarkable.
Method for preparing alpha, beta-unsaturated carboxylic acid by reacting alkenyl boron compound with carbon dioxide under catalysis of cuprous halide
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Paragraph 0069-0070, (2020/06/17)
The invention discloses a method for preparing alpha, beta-unsaturated carboxylic acid through a carboxylation reaction of an alkenyl boron compound and carbon dioxide under the catalysis of cuprous halide. According to the method, carbon dioxide is used as a C1 source, the cuprous halide is adopted for catalysis, and alkoxide serves as alkali to react in an organic solvent, so the method is simple and easy to implement, has a wide substrate application range, converts various alkenyl boron compounds such as alkenyl boric acid, alkenyl borate and borate into corresponding alpha, beta-unsaturated carboxylic acid under mild conditions, and has a very high yield. The obtained product alpha, beta-unsaturated carboxylic acid is an important intermediate for preparing fine chemical products suchas perfumes, insecticides and the like.
Carboxylation of Alkenyl Boronic Acids and Alkenyl Boronic Acid Pinacol Esters with CO2 Catalyzed by Cuprous Halide
Hong, Junting,Nayal, Onkar S.,Mo, Fanyang
supporting information, p. 2813 - 2818 (2020/05/16)
A cuprous halide catalysed carboxylation of alkenyl boronic acids and alkenyl boronic acid pinacol esters under CO2, affording the corresponding α, β-unsaturated carboxylic acids in good yield, has been developed. The potassium (E)-trifluoro(styryl)borate is also compatible with this reaction. This simple and efficient copper(I) catalytic system showed good functional group tolerance.
A comparative study on degradation of complex malathion organophosphate using of Escherichia coli IES-02 and a novel carboxylesterase
Ansari, Asma,Iqbal, Sajid,Khan, Moazzam Ali,Qader, Shah Ali Ul,Sattar, Hafsa,Sirajuddin, Sadia
, p. 445 - 455 (2020/01/08)
Malathion organophosphates considered as the major constituent of herbicides, pesticides and insecticides. Extensively used in agricultural, horticultures and for numerous household applications contributes to precedence organic pollutants leading antagonistic effects on human health and environment. Therefore detoxification of malathion from contaminated site is of general interest. Simultaneously it is very emerging to isolated novel indigenous microbial strains from contaminated site with a record of pesticide application. In this study Escherichia coli IES-02 isolated from malathion contaminant effluent and the strain showed maximum efficiency in malathion degradation that utilized it as the sole source of carbon. Carboxylesterase (33.0, 30.0, 28.0 kDa) were purified (1685.71 U/mg) from Escherichia coli IES-02 showed significant results in malathion degradation approximately 81% within 20 min as compared with Escherichia coli IES-02 cells within 4 h (99.0 to 95.0%) into monocarboxylic acid and diacid derivatives. The generation time of Escherichia coli was also observed at 60 min with 0.1 ppm, 68 min with 0.5 ppm, 74.5 min with 2.0 ppm and 91.37 min with 50 ppm of malathion. The degradation rate and transformation metabolites were estimated by Gas Chromatography-Mass Spectrometry respectively. Malathion metabolites pathway proposed in this study which revealed the potential application against lethal environmental pollution.
DRUGS AND COMPOSITIONS FOR OCULAR DELIVERY
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Page/Page column 160; 161, (2019/07/19)
New prodrugs of therapeutically active compounds, including oligomeric prodrugs of ethacrynic acid, and compositions to treat medical disorders, for example glaucoma, a disorder or abnormality related to an increase in intraocular pressure (IOP), a disorder requiring neuroprotection, age-related macular degeneration, or diabetic retinopathy. Also a method for the controlled administration of timolol to a patient in need thereof, such as a human, comprising administering a prodrug of timolol in a microparticle in vivo, wherein the timolol prodrug containing microparticle exhibits in vitro drug release kinetics in an aqueous solution at a pH between 6-8 at body temperature of a substantially consistent release of at least 60% timolol itself by molar ratio to the prodrug of timolol or an intermediate metabolite thereof over at least 100 days.
DRUGS AND COMPOSITIONS FOR THE TREATMENT OF OCULAR DISORDERS
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Page/Page column 245; 383, (2018/10/19)
The present invention provides new prodrugs of therapeutically active compounds, including oligomeric prodrugs, and compositions to treat medical disorders, for example glaucoma, a disorder or abnormality related to an increase in intraocular pressure (IOP), a disorder requiring neuroprotection, age-related macular degeneration, or diabetic retinopathy.
Preparation method of ethyl 4-(3,4-dimethoxyphenyl)-4-oxo-2-butenoate
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Paragraph 0027; 0029; 0038; 0041; 0042; 0043, (2018/11/03)
The invention relates to a preparation method of ethyl 4-(3,4-dimethoxyphenyl)-4-oxo-2-butenoate, and belongs to the technical field of chemical reagent synthesis. The preparation method comprises thefollowing steps: firstly performing an esterification reaction on maleic anhydride and ethanol, then performing a transposition reaction to obtain monoethyl fumarate, then performing a reaction on the monoethyl fumarate and sulfoxide chloride to obtain monoethyl monoacyl chloride fumarate, finally performing a reaction on the monoethyl monoacyl chloride fumarate and 1,2-dimethoxybenzene to obtaina target product ethyl 4-(3,4-dimethoxyphenyl)-4-oxo-2-butenoate, and refining to obtain a refined product. By the preparation method, a reaction product in each step is relatively high in yield andpurity, the finally prepared refined product is also high in yield and purity, and raw materials are simple, easy to obtain and low in cost; in addition, the preparation method is easy to operate, impurities in the product are easily separated and removed, and the refined product has the purity of 99% or above and fully meets requirements of customers for a medical purpose.
Synthesis of α,β-unsaturated esters of perfluoropolyalkylethers (PFPAEs) based on hexafluoropropylene oxide units for photopolymerization
Bonneaud, Céline,Decostanzi, Mélanie,Burgess, Julia,Trusiano, Giuseppe,Burgess, Trevor,Bongiovanni, Roberta,Joly-Duhamel, Christine,Friesen, Chadron M.
, p. 32664 - 32671 (2018/10/15)
α,β-unsaturated esters are usually synthesized for polymer applications. However, the addition of maleate (cis-configuration) to a fluorinated moiety is challenging due to its potential isomerization during esterification. Various synthetic routes were attempted and led to very low conversion or side-products. The immiscibility of both reagents combined with an easy isomerization or attack on the double bond were potential explanations. In this paper, the synthesis of maleates oligo(hexafluoropropylene oxide) is reported by Steglich esterification and the reaction conditions are discussed depending on the molecular weight of the fluorinated moieties. After UV-curing, hydrophobic polymers were obtained by copolymerization with vinyl ethers by electron acceptor-donor systems.
Synthesis, DFT and antimicrobial activity assays in vitro for novel cis/trans-but-2-enedioic acid esters
Ma, Yan-Long,Zhou, Ru-Jin,Zeng, Xing-Ye,An, Ya-Xiong,Qiu, Song-Shan,Nie, Li-Jun
, p. 226 - 234 (2014/03/21)
Six novel cis/trans-but-2-enedioic acid esters had been synthesized to discover the new bioactive molecules that could kill food-related bacteria and fungi. Their structures were analyzed by melting point, LC-MS, 1H NMR and 13C NMR. 4-(Methoxycarbonyl) phenyl ethyl fumarate (6b) was also characterized by single-crystal X-ray diffraction. Their antimicrobial activities were evaluated in vitro by measuring the minimal inhibitory concentration (MIC). Compared with the single monomethyl fumarate and methyl 4-hydroxybenzoate, these compounds had stronger antimicrobial activity against all the eight microorganisms. Among the antibacterial and antifungal compounds, 4-(methoxycarbonyl) phenyl methyl fumarate (6a) showed the best antimicrobial activity. The electronic properties of these compounds were calculated by the density functional theory (DFT) method with 6-31G (d, p) basis set. DFT studies indicated that molecular electrostatic potential (MEP) map, ELUMO, energy gap, electronegativity and electrophilicity index could be helpful to understand the various antimicrobial activities among these compounds. The antimicrobial activity of compound 6a was evaluated in vitro against Salmonella choleraesuis subsp. choleraesuis, Lactococcus lactis subsp. lactis and Saccharomyces cerevisiae by time-kill, and it was found that compound 6a exhibited significant microbiocidal activity against the three microorganisms.
