70067-75-3Relevant academic research and scientific papers
Synthetic method 4 - alkoxyphenol compounds
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Paragraph 0058-0060, (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.
EED-Targeted PROTACs Degrade EED, EZH2, and SUZ12 in the PRC2 Complex
Argyrou, Argyrides,Bagal, Sharan,Bednarski, Emma,Bloecher, Andrew,Castaldi, M. Paola,Chiarparin, Elisabetta,Code, Erin,Drew, Lisa,Fawell, Stephen,Gao, Ning,Hsu, Jessie Hao-Ru,Jacques, Kelly,Kawatkar, Sameer,O’ Donovan, Daniel H.,Pachl, Fiona,Rasmusson, Timothy,Rawlins, Philip,Read, Jon,Robinson, James,Shen, Minhui,Tomlinson, Ronald,Wilson, David M.,Woods, Haley,Zhu, Xiahui
, p. 41 - 46 (2020/01/13)
Deregulation of the PRC2 complex, comprised of the core subunits EZH2, SUZ12, and EED, drives aberrant hypermethylation of H3K27 and tumorigenicity of many cancers. Although inhibitors of EZH2 have shown promising clinical activity, preclinical data sugge
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.
ARYL PYRIMIDINE DERIVATIVES, PREPARATION METHODS AND PHARMACEUTICAL USES THEREOF
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Page/Page column 8, (2011/02/15)
The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof. Various substituents in the formula (I) are as defined in the specification. The present invention also relates to a pharmaceutical composition comprising the compound of formula (I), the preparation method of compound of formula (I), and the use of the compound for the preparation of a medicament for treating and/or preventing human peroxisome proliferators activated receptor δ (hPPARδ)-associated diseases and risk factors.
ARYL PYRIMIDINE DERIVATIVES, PREPARATION METHODS AND PHARMACEUTICAL USES THEREOF
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Page/Page column 13, (2010/06/11)
The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof. Various substituents in the formula (I) are as defined in the specification. The present invention also relates to a pharmaceutical composition comprising the compound of formula (I), the preparation method of compound of formula (I), and the use of the compound for the preparation of a medicament for treating and/or preventing human peroxisome proliferators activated receptor δ (hPPARδ) -associated diseases and risk factors.
FUNCTIONALIZED DIPHENOLICS AND ABSORBABLE POLYMERS THEREFROM
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Page/Page column 20, (2008/06/13)
The present invention relates to dephenolic compounds, an example of which is shown below, which are functionalized, and polymers formed from the same. Polymers formed from the functionalized diphenolics are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.
COMPOUNDS AND COMPOSITIONS AS PPAR MODULATORS
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Page/Page column 41-42, (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.
COMPOUNDS AND COMPOSITIONS AS PPAR MODULATORS
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Page/Page column 36, (2008/06/13)
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.
Design and synthesis of potent and subtype-selective PPARα agonists
Desai, Ranjit C.,Metzger, Edward,Santini, Conrad,Meinke, Peter T.,Heck, James V.,Berger, Joel P.,MacNaul, Karen L.,Cai, Tian-Quan,Wright, Samuel D.,Agrawal, Arun,Moller, David E.,Sahoo, Soumya P.
, p. 1673 - 1678 (2007/10/03)
Beginning with a moderately potent PPARγ agonist 9, a series of potent and highly subtype-selective PPARα agonists was identified through a systematic SAR study. Based on the results of the efficacy studies in the hamster and dog models of dyslipidemia and the desired pharmacokinetic data, the optimized compound 39 was selected for further profiling.
