99103-80-7Relevant academic research and scientific papers
Heterobivalent Ligand for the Adenosine A2A-Dopamine D2Receptor Heteromer
Casajuana-Martin, Nil,Pardo, Leonardo,Pulido, Daniel,Royo, Miriam,Casadó, Vicent,Casadó-Anguera, Verònica,Ferré, Sergi,Gómez-Autet, Marc,Llopart, Natàlia,Moreno, Estefanía
supporting information, (2022/01/20)
A G protein-coupled receptor heteromer that fulfills the established criteria for its existence in vivo is the complex between adenosine A2A (A2AR) and dopamine D2 (D2R) receptors. Here, we have designed and synthesized heterobivalent ligands for the A2AR
Site-Selective C?H Oxygenation via Aryl Sulfonium Salts
Sang, Ruocheng,Korkis, Stamatis E.,Su, Wanqi,Ye, Fei,Engl, Pascal S.,Berger, Florian,Ritter, Tobias
supporting information, p. 16161 - 16166 (2019/11/03)
Herein, we report a two-step process forming arene C?O bonds in excellent site-selectivity at a late-stage. The C?O bond formation is achieved by selective introduction of a thianthrenium group, which is then converted into C?O bonds using photoredox chemistry. Electron-rich, -poor and -neutral arenes as well as complex drug-like small molecules are successfully transformed into both phenols and various ethers. The sequence differs conceptually from all previous arene oxygenation reactions in that oxygen functionality can be incorporated into complex small molecules at a late stage site-selectively, which has not been shown via aryl halides.
A singlet oxygen approach to oxaspirocycles
Jones, Kevin M.,Hillringhaus, Tim,Klussmann, Martin
supporting information, p. 3294 - 3297 (2013/06/27)
A method for the preparation of oxygen containing spirocycles using singlet oxygen is reported. A series of phenols were converted into the corresponding peroxy-cyclohexadienone derivatives by irradiation with visible light in the presence of a sensitizer and oxygen. The resulting peroxides could be converted into ether and lactone spirocycles in one or two steps. The synthesis of the oxaspirocycles from the phenols can also be performed in a one-pot fashion, avoiding the isolation of the peroxide intermediates.
2-Phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors: A study on the importance of modifications at the side chain on the activity
Shen, Yanhong,Sheng, Rong,Zhang, Jing,He, Qiaojun,Yang, Bo,Hu, Yongzhou
, p. 7646 - 7653 (2008/12/23)
As a part of our project aimed at developing new agents of potential application in AD, a new series of 2-phenoxy-indan-1-one derivatives which possess alkylamine side chain were designed, synthesized, and evaluated for their inhibitory activity against AChE and BuChE. Most of the compounds were found to inhibit AChE in the nanomolar range. The optimum inhibitor 3g exhibited 34-fold increase in AChE inhibition than donepezil and displayed neuroprotective effect against H2O2-induced cell death.
Interaction of functionally-substituted 4-alkyl-2,6-di-tert-butylphenols with hydrohalic acids
Prosenko,Skorobogatov,Dyubchenko,Pinko,Kandalintseva,Shakirov,Pokrovsky
, p. 1119 - 1124 (2008/09/18)
Reactions of 4-alkyl-2,6-di-tert-butylphenols containing OH, SH, COOH, and COOMe groups in their para substituents with hydrogen chloride and hydrohalic acids were studied. One-step transformations of 2,6-di-tert-butyl-4-(ω- hydroxyalkyl)phenols to the corresponding 4-(ω-halogenoalkyl)phenols, as well as of 3-(3,5-di-tert-butyl-4-hydroxyphenyl)propionic acid and its esters to phloretic acid were proposed. 4-(3-Mercaptopropyl)phenol upon heating with conc. HBr undergoes condensation to 3-(4-hydroxyphenyl)propyl 4-(3-mercaptopropyl)phenyl sulfide as the main product.
PROPIONAMIDE DERIVATIVES USEFUL AS ANDROGEN RECEPTOR MODULATORS
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Page 53, (2010/02/10)
Compounds of formula (I) wherein R1 to R4, X and A are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as tissue-selective androgen receptor modulators (SARM) and are useful in hormonal therapy, e.g. in the treatment or prevention of male hypogonadism and age-related conditions such as andropause.
