60075-04-9Relevant academic research and scientific papers
Synthetic method 4 - alkoxyphenol compounds
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Paragraph 0064-0066, (2021/09/29)
The invention discloses a synthetic method of 4 - alkoxyphenol compounds, and belongs to the field of organic chemical synthesis. The method is as follows: An aryl alkyl ether compound is added to the sealing tube. The catalyst dimerization acetic acid rhodium and the oxidizing agent iodobenzene diethyl ester are added, a solvent trifluoroacetic anhydride is added, and the 4 -alkoxyphenol compound is prepared by heating reaction. To the invention, high regioselectivity direct hydroxylation of the aryl alkyl ether compound is realized, the application range of the substrate is wide, the yield is high, the activity after amplification reaction does not significantly decay, and higher yield is still obtained. The utility model has good practicability and industrial application prospect.
Para -Selective hydroxylation of alkyl aryl ethers
Zhu, Runqing,Sun, Qianqian,Li, Jing,Li, Luohao,Gao, Qinghe,Wang, Yakun,Fang, Lizhen
supporting information, p. 13190 - 13193 (2021/12/16)
para-Selective hydroxylation of alkyl aryl ethers is established, which proceeds with a ruthenium(ii) catalyst, hypervalent iodine(iii) and trifluoroacetic anhydride via a radical mechanism. This protocol tolerates a wide scope of substrates and provides a facile and efficient method for preparing clinical drugs monobenzone and pramocaine on a gram scale.
6-chlorobenzoxazoloxy phenoxyacrylamide compounds and application thereof
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Paragraph 0058-0061, (2018/06/04)
The invention discloses 6-chlorobenzoxazoloxy phenoxyacrylamide compounds and an application thereof as herbicides; the compounds are represented by the general formula (I), wherein W is selected fromC1-4 alkylene. The compounds not only have excellent he
Method for synthesizing herbicide clodinafop-propargyl key intermediate
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Paragraph 0049, (2018/11/27)
The invention discloses a method for synthesizing a herbicide clodinafop-propargyl key intermediate. According to the method, methyl 2-chloropropionate and hydroquinone are used as starting raw materials, under the catalytic action of inorganic alkali, nucleophilic substitution reaction is conducted, and methyl (R,S)-2-(4-hydroxyphenoxy)propionate is obtained; the generated methyl (R,S)-2-(4-hydroxyphenoxy)propionate is subjected to resolution hydrolysis reaction under the action of aspergillus oryzae WZ007, and a methyl (R)-(+)-2-(4-hydroxyphenoxy)propionate product is obtained; the generatedproduct is subjected to hydrolysis reaction continuously to obtain a target product R(+)-2-(4-hydroxyphenoxy)propionic acid. The synthesis method is simple; in the synthesis process, thalli of the aspergillus oryzae WZ007 are used for catalyzing selective hydrolysis of a methyl (R,S)-2-(4-hydroxyphenoxy)propionate substrate, thus the R-configuration ester and the S-configuration acid are obtained, the purpose of resolution is achieved, moreover, the raw materials of the method are cheap, the production cost is low, and the economic performance is good, so that the method has good applicationprospects.
6-chlorobenzoxazol-oxyphenoxy propionate compound and application thereof
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Paragraph 0066-0069, (2017/08/18)
The invention belongs to the field of herbicides and particularly relates to a 6-chlorobenzoxazol-oxyphenoxy propionate compound and application thereof. The compound is shown in a general formula (I). The compound provided by the invention not only has e
Synthesizing method for (R)-(+)-2-(4-hydroxy phenoxy) methyl propionate
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Paragraph 0005; 0016, (2017/04/03)
The invention discloses a synthesizing method for (R)-(+)-2-(4-hydroxy phenoxy)methyl propionate.The synthesizing method comprises the following steps that firstly, hydroquinone and a sodium hydroxide aqueous solution are put into a reaction kettle for a reaction, and a mixed solution containing p-hydroxyl sodium phenolate is generated; secondly, methyl 2-chloropropionate is added into the reaction kettle for a substitution reaction, and a mixed solution containing (R)-(+)-2-(4-hydroxy phenoxy)methyl propionate is generated; thirdly, an extraction solvent is added in the reaction kettle for extraction laying treatment, and then oil layer distillation treatment is carried out; fourthly, the mixed solution, obtained after oil layer distillation treatment, containing (R)-(+)-2-(4-hydroxy phenoxy)methyl propionate is cooled, crystallized, centrifuged and dried.The synthesizing procedures of the synthesizing method are simple, the product quality is good, the yield is high, and obtained MAQ is a white crystalline solid.
Synthesis and biological evaluation of phenoxyacetic acid derivatives as novel free fatty acid receptor 1 agonists
Wang, Xuekun,Zhao, Tianxiao,Yang, Baowei,Li, Zheng,Cui, Jian,Dai, Yuxuan,Qiu, Qianqian,Qiang, Hao,Huang, Wenlong,Qian, Hai
, p. 132 - 140 (2015/02/18)
Free fatty acid receptor 1 (FFA1) is a new potential drug target for the treatment of type 2 diabetes because of its role in amplifying glucose-stimulated insulin secretion in pancreatic β-cell. In the present studies, we identified phenoxyacetic acid derivative (18b) as a potent FFA1 agonist (EC50 = 62.3 nM) based on the structure of phenylpropanoic acid derivative 4p. Moreover, compound 18b could significantly improve oral glucose tolerance in ICR mice and dose-dependently reduced glucose levels in type 2 diabetic C57BL/6 mice without observation of hypoglycemic side effect. Additionally, compound 18b exhibited acceptable PK profiles. In summary, compound 18b with ideal PK profiles exhibited good activity in vitro and in vivo, and might be a promising drug candidate for the treatment of diabetes mellitus.
Resolution of (R, S)-ethyl-2-(4-hydroxyphenoxy) propanoate using lyophilized mycelium of Aspergillus oryzae WZ007
Zheng, Jian-Yong,Wu, Jia-Yu,Zhang, Yin-Jun,Wang, Zhao
, p. 62 - 66 (2013/10/01)
The mycelium of Aspergillus oryzae WZ007 was successfully developed to kinetic resolution of (R, S)-ethyl-2-(4-hydroxyphenoxy) propanoate ((R, S)-EHPP) for production of (R)-ethyl-2-(4-hydroxyphenoxy) propanoate ((R)-EHPP). The key biocatalytic process parameters (pH, temperature, rotation speed and substrate concentration) were optimized. Under the optimum conditions, the optical purity of (R)-EHPP was improved up to >99% when the conversion was above 49%. A. oryzae WZ007 whole-cell lipase exhibited high reaction capacity, enantioselectivity and good reusability. The tolerable substrate concentration was 0.5 mol/L, and dry mycelium of A. oryzae WZ007 maintains over 80% of its initial activity after eight repeating cycles. Therefore the enzymatic preparation of (R)-EHPP route was suitable for industrial application.
COMPOUNDS AND COMPOSITIONS AS PPAR MODULATORS
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Page/Page column 54, (2010/11/27)
The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated Receptor (PPAR) families.
A novel synthesis and herbicidal activity of fluorine-containing pyrazolo[3,4-d]pyrimidin-4-one derivatives
Liu, Hui,Wang, Hong-Qing,Ding, Ming-Wu,Liu, Zhao-Jie,Xiao, Wen-Jing
, p. 1584 - 1590 (2008/09/18)
The 6-(4-alkoxycarbonylalkoxy)phenoxy-3-alkylthio-5-(fluoro-substituted)phenyl-1-phenylpyrazolo[3,4-d]pyrimidin-4-ones 6 have been successfully synthesized via a tandem aza-Wittig and annulation reactions of the corresponding iminophosphorances 4, aromatic isocyanate, and substituted phenols 2 in 59-69% isolated yields using actonitrile as solvent. These novel compounds 6 could be oxidized to sulfones 7 by hydrogen peroxide in satisfactory yields (57-93%). Their structures were clearly verified by spectroscopic data (IR, 1H NMR, 13C NMR, MS, Elemental analysis or X-ray diffraction crystallography). The results of preliminary bioassay indicated that these compounds possess herbicidal activity against the root of rape and barnyard grass.
