- Substituted diaryl ether compounds as retinoic acid-related orphan Receptor-γt (RORγt) agonists
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The discovery of a series of substituted diarylether compounds as retinoic acid related orphan receptor γt (RORγt) agonists is described. Compound 1 was identified from deck mining as a RORγt agonist. Hit-to-lead optimization led to the identification of
- Ruan, Zheming,Park, Peter K.,Wei, Donna,Purandare, Ashok,Wan, Honghe,O'Malley, Daniel,Stachura, Sylwia,Perez, Heidi,Cavallaro, Cullen L.,Weigelt, Carolyn A.,Sack, John S.,Ruzanov, Max,Khan, Javed,Gururajan, Murali,Wong, Jessica J.,Huang, Yanling,Yarde, Melissa,Li, Zhuyin,Chen, Cliff,Sun, Huadong,Borowski, Virna,Xie, Jenny H.,Anthony, Monique,Agler, Michele,Fink, Brian E.,Harikrishnan, Lalgudi S.
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- Synthetic method 4 - alkoxyphenol compounds
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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.
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Paragraph 0079-0081
(2021/09/29)
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- Para -Selective hydroxylation of alkyl aryl ethers
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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.
- Zhu, Runqing,Sun, Qianqian,Li, Jing,Li, Luohao,Gao, Qinghe,Wang, Yakun,Fang, Lizhen
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supporting information
p. 13190 - 13193
(2021/12/16)
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- Rational Design of Potent and Selective Inhibitors of an Epoxide Hydrolase Virulence Factor from Pseudomonas aeruginosa
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The virulence factor cystic fibrosis transmembrane conductance regulator (CFTR) inhibitory factor (Cif) is secreted by Pseudomonas aeruginosa and is the founding member of a distinct class of epoxide hydrolases (EHs) that triggers the catalysis-dependent
- Kitamura, Seiya,Hvorecny, Kelli L.,Niu, Jun,Hammock, Bruce D.,Madden, Dean R.,Morisseau, Christophe
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supporting information
p. 4790 - 4799
(2016/06/13)
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- Re2O7 catalyzed dienone-phenol rearrangement
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The dienone-phenol rearrangement of 4,4-disubstituted cyclohexadienones catalyzed by Re2O7 has been described. Multi-substituted phenols can be efficiently obtained in good to excellent yields by employing this catalytic protocol.
- Xia, Zilei,Hu, Jiadong,Shen, Zhigao,Yao, Qizheng,Xie, Weiqing
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p. 38499 - 38502
(2015/06/24)
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- SUBSTITUTED ANILIDE LIGANDS FOR THE THYROID RECEPTOR
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Novel thyroid receptor ligands are provided having the general formula I wherein X, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12. and R13 are as defined herein. In addition, a method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolic dysfunction or which are dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.
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- Process for the preparation of aniline-derived thyroid receptor ligands
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Provided are processes for the synthesis of aniline derivatives, specifically certain aniline derivatives which have activity as thyroid receptor ligands.
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