- ISOTOPIC THYROMIMETIC COMPOUNDS
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Isotopic compounds are provided that function as thyromimetics, which compounds have utility for treating diseases such as neurodegenerative disorders. Pharmaceutical compositions containing such compounds are also provided, as are methods of their use an
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Paragraph 00146
(2021/12/28)
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- Copper-catalysed low-temperature water-gas shift reaction for selective deuteration of aryl halides
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The introduction of deuterium atoms into organic compounds is of importance for basic chemistry, material sciences, and the development of drugs in the pharmaceutical industry, specifically for identification and quantification of metabolites. Hence, methodologies for the synthesis of selectively labelled compounds continue to be a major area of interest for many scientists. Herein, we present a practical and stable heterogeneous copper catalyst, which permits for dehalogenative deuterationviawater-gas shift reaction at comparably low temperature. This novel approach allows deuteration of diverse (hetero)aryl halides with good functional group tolerance, and no reduction of the aromatic rings or other easily reducible formyl and cyano groups. Multi-gram experiments show the potential of this method in organic synthesis and medicinal chemistry.
- Bartling, Stephan,Beller, Matthias,Bourriquen, Florian,Junge, Kathrin,Li, Wu,Liu, Weiping,Qu, Ruiyang,Rockstroh, Nils
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p. 14033 - 14038
(2021/11/12)
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- Shifted Selectivity in Protonation Enables the Mild Deuteration of Arenes through Catalytic Amounts of Bronsted Acids in Deuterated Methanol
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Taking advantage of the "differentiating effect"of the solvent methanol, deuterations of electron-rich aromatic systems can be carried out under mild acid catalysis and thus under far milder conditions than known so far. The exceptional functional group t
- Fischer, Oliver,Hubert, Anja,Heinrich, Markus R.
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p. 11856 - 11866
(2020/10/23)
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- A substituted heteroaryl compounds and compositions containing such compounds and use thereof (by machine translation)
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The present invention provides a substituted heteroaryl compounds and compositions containing such compounds and its use, the invention discloses a formula (I) indicated by the heteroaryl compound, or its crystalline form, a pharmaceutically acceptable salt, prodrug, stereoisomer, hydrate or compound solvent. The invention of monocyclic the base states compounds and compositions containing such compounds may be used to modulate hypoxia inducible factor (HIF) and/or endogenous erythropoietin (EPO), but also has good pharmacokinetic parameter characteristic, can improve the compound in animal drug concentration, in order to improve the effect of drugs and safety. (by machine translation)
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Paragraph 0088; 0089-0090
(2017/04/19)
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- A simple and cost-effective method for the regioselective deuteration of phenols
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A highly effective and operationally simple method for the deuteration of phenols using NaOH as a catalyst and D2O as the deuterium source is presented. A high regioselectivity for the ortho and/or para hydrogens relative to the oxygen atom was
- Zhan, Miao,Xu, Ruixue,Tian, Ye,Jiang, Hongxia,Zhao, Lifeng,Xie, Yongmei,Chen, Yuanwei
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supporting information
p. 3370 - 3373
(2015/05/20)
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- Intramolecular annulation of aromatic rings with N-sulfonyl 1,2,3-triazoles: Divergent synthesis of 3-methylene-2,3-dihydrobenzofurans and 3-methylene-2,3-dihydroindoles
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The controllable synthesis of 3-methylene-2,3-dihydrobenzofurans 2 and 3-methylene-2,3-dihydroindoles 5 has been developed through Rh-catalyzed intramolecular annulation of aromatic rings with azavinyl carbenes. This journal is
- Tang, Xiang-Ying,Zhang, Yong-Sheng,He, Lv,Wei, Yin,Shi, Min
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supporting information
p. 133 - 136
(2015/01/09)
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- METHOD FOR PRODUCING AROMATIC HYDROCARBON
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PROBLEM TO BE SOLVED: To provide a method for producing an aromatic compound having deutrium, excellent in an economical property and an all purpose property. SOLUTION: This method for producing the aromatic compound is characterized by producing a compound having deutrium at at least one of selected positions among ortho-, meta- and para-positions by performing a substitution reactions on hydrogen directly bonded to a benzene ring of a compound expressed by formula (1) [wherein, X is a substituent having an electron-donating property] from deutrium to hydrogen or from hydrogen to deutrium.
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Page/Page column 23-24
(2008/06/13)
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- Efficient H-D exchange of aromatic compounds in near-critical D2O catalysed by a polymer-supported sulphonic acid
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Hydrogen atom exchange of aromatic compounds in neutral near-critical D2O has been improved by using a polymer-supported sulphonic acid catalyst. Phenol, aniline, quinoline, and substituted aromatic hydrocarbons are selectively ring-perdeuterated in high yields with insignificant by-product formation at 325 °C for 24 h in D2O/Deloxan.
- Boix, Carmen,Poliakoff, Martyn
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p. 4433 - 4436
(2007/10/03)
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- Aromatization of Arene 1,2-Oxides. 1-(Trimethylsilyl)benzene 1,2-Oxide
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Aromatization of 1-(trimethylsilyl)benzene 1,2-oxide (1) affords a mixture of o-(trimethylsilyl)phenol and phenol, the ratio of which is pH dependent.Aromatization of -1-(trimethylsilyl)benzene 1,2-oxide gave the following results. (1) At pH 1.1 or 7 all the deuterium label in o-(trimethylsilyl)phenol was para to the hydroxyl group. (2) At pH 1.1 the phenol formed was exclusively phenol, but at pH 7 it was 70-75percent phenol and 25-30percent phenol.The pathway of the aromatization reaction is discussed.
- Epp, James E. Van,Boyd, Derek R.,Berchtold, Glenn A.
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p. 1817 - 1820
(2007/10/02)
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