1467-05-6Relevant articles and documents
Efficient selective synthesis of ethylbenzonitriles
Xie, Guangyong,Zhang, Aiqing
, p. 375 - 379 (2012)
Ethylbenzonitriles were synthesized by selective gas-phase ammoxidation of ethylbenzyl chlorides prepared by chloromethylation of ethylbenzene in good yields and almost 100% selectivity at ca. 200 °C for the first time.Copyright Taylor & Francis Group, LLC.
Cu(II)/Cu(0)@UiO-66-NH2: Base metal@MOFs as heterogeneous catalysts for olefin oxidation and reduction
Wang, Jian-Cheng,Hu, Yu-Hong,Chen, Gong-Jun,Dong, Yu-Bin
, p. 13116 - 13119 (2016)
Two copper-loaded MOF materials, namely Cu(ii)@Ui-O-66-NH2 (1) and Cu(0)@UiO-66-NH2 (2), are reported. They can, respectively, serve as highly efficient heterogeneous catalysts for olefin oxidation and hydrogenation under mild conditions. Complete styrene hydrogenation occurs in 15 min at ambient temperature with quantitative yield.
Structure-guided optimization of 1H-imidazole-2-carboxylic acid derivatives affording potent VIM-Type metallo-β-lactamase inhibitors
Yan, Yu-Hang,Li, Wenfang,Chen, Wei,Li, Chao,Zhu, Kai-Rong,Deng, Ji,Dai, Qing-Qing,Yang, Ling-Ling,Wang, Zhenling,Li, Guo-Bo
, (2021/11/17)
Production of metallo-β-lactamases (MBLs) in bacterial pathogens is an important cause of resistance to the ‘last-resort’ carbapenem antibiotics. Development of effective MBL inhibitors to reverse carbapenem resistance in Gram-negative bacteria is still needed. We herein report X-ray structure-guided optimization of 1H-imidazole-2-carboxylic acid (ICA) derivatives by considering how to engage with the active-site flexible loops and improve penetration into Gram-negative bacteria. Structure-activity relationship studies revealed the importance of appropriate substituents at ICA 1-position to achieve potent inhibition to class B1 MBLs, particularly the Verona Integron-encoded MBLs (VIMs), mainly by involving ingenious interactions with the flexible active site loops as observed by crystallographic analyses. Of the tested ICA inhibitors, 55 displayed potent synergistic antibacterial activity with meropenem against engineered Escherichia coli strains and even intractable clinically isolated Pseudomonas aeruginosa producing VIM-2 MBL. The morphologic and internal structural changes of bacterial cells after treatment further demonstrated that 55 crossed the outer membrane and reversed the activity of meropenem. Moreover, 55 showed good pharmacokinetic and safety profile in vivo, which could be a potential candidate for combating VIM-mediated Gram-negative carbapenem resistance.
Preparation method of 4-ethylbenzyl chloride
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Paragraph 0027-0029, (2021/11/26)
The invention discloses a preparation method of 4-ethylbenzyl chloride, and belongs to the technical field of organic synthesis. The method comprises the following steps: chloromethylating ethylbenzene serving as a raw material with acetal, chlorosulfonic acid and lewis acid under the catalytic action to obtain 4-ethylbenzyl chloride. According to the method, the catalyst can be recycled and reused, isomers are few, separation is relatively easier, the yield is high, the content of the obtained product is larger than 99%, and potential industrial amplification prospects are achieved.
An efficient and convenient chloromethylation of some aromatic compounds catalyzed by zinc iodide
Tang, Jian,Liu, Hongtao,Zhou, Jing,Zhang, Xingxian
, p. 34 - 38 (2019/06/21)
Treatment of a series of aromatic hydrocarbons and O-carbethoxy phenol substrates with a mixture of chlorosulfonic acid and dimethoxymethane in CH2Cl2 catalyzed by zinc iodide affords the corresponding chloromethyl derivatives in good to excellent yields.
A practical and convenient Blanc-type chloromethylation catalyzed by zinc chloride under solvent-free conditions
Tang, Jian,Liu, Hongtao,He, Kailun,Zhang, Xingxian
, p. 925 - 932 (2019/03/17)
Chloromethylation of various aromatic hydrocarbons and substituted phenolic derivatives with dimethoxymethane and chlorosulfonic acid was carried out in the presence of 10 mol% of ZnCl2 in a mild and efficient manner under solvent-free conditions. In addition, 2,6-dimethyltyrosine was synthesized in high yield via this protocol.
A method of preparing intermediates sea breeze aldehyde
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Paragraph 0056-0060, (2017/02/09)
The invention discloses a method of preparing a floralozone intermediate. Under the action of an aqueous sulfuric acid solution and a quaternary ammonium salt as a phase transfer catalyst, by controlling the reaction temperature, hydrogen chloride gas is continuously fed into a reaction system containing ethylbenzene and paraformaldehyde so as to perform chloromethylation of the ethylbenzene, and ethylbenzyl chloride with a purity higher than 95% and a yield being 85-94% is finally prepared. By adoption the ethylbenzyl chloride as the intermediate, floralozone can be prepared by condensing the intermediate and isobutyraldehyde.
A method of preparing sea breeze aldehyde
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Paragraph 0088-0092, (2017/02/23)
The invention discloses a preparation method of floralozone. The preparation method comprises the steps of dropwise adding isobutyraldehyde into an ethyl benzyl chloride contained reaction system through controlling the reaction temperature under the action that sodium hydroxide and quaternary ammonium salt compounds are used as phase transfer catalysts, and finally, preparing at the yield of 70-85% to obtain floralozone with the content up to more than 94%. The preparation method of floralozone, disclosed by the invention, is low in yield of three wastes, strong in process operability and low in cost.
An inexpensive and convenient procedure for chloromethylation of aromatic hydrocarbons by phase transfer catalysis in aqueous media
Hu, Yu Lin,Lu, Ming,Ge, Qiang,Wang, Peng Cheng,Zhang, Sheng Bin,Lu, Ting Ting
experimental part, p. 97 - 102 (2010/08/05)
Reaction of aromatic hydrocarbons catalyzed by a novel catalytic system consisting of zinc chloride, acetic acid, sulfuric acid and PEG-800 in aqueous media under PTC conditions results in chloromethylation in good to excellent yield.
BENZODIAZEPINONE COMPOUNDS USEFUL IN THE TREATMENT OF SKIN CONDITIONS
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Page/Page column 17, (2009/05/28)
The present invention provides a family of benzodiazepinone compounds and pharmaceutical compositions thereof. The present invention also provides methods of treating certain skin conditions, e.g., atopic dermatitis, rosacea, or psoriasis, by administering a benzodiazepinone and methods of reducing the proliferation of keratinocyte cells by exposing such cells to a benzodiazepinone.
