2357-52-0Relevant academic research and scientific papers
The Synthesis and Transition Temperatures of Benzoate Ester Derivatives of 2-Fluoro-4-hydroxy- and 3-Fluoro-4-hydroxybenzonitriles
Kelly, Stephen M.
, p. 1572 - 1579 (1984)
The synthesis and the liquid-crystal temperatures of sixty 4-cyano-2-flurophenyl and 4-cyano-3-fluorophenyl 4-substituted benzoates are described.The nematic-isotropic liquid transition temperatures of most of these novel esters are only marginally lower than those of the corresponding esters containing an H-atom in place of the F-substituent.In several instances, the clearing points of the F-substituted-phenyl esters are higher than those of the non-substituted-phenyl esters.The nematic ranges of several new esters are markedly broader than those of the analogous non-F-susbstituted-phenyl esters.
Organophotochemical SNAr Reactions of Mildly Electron-Poor Fluoroarenes
Burton, Jonathan W.,Genovino, Julien,Lian, Yajing,Monck, Nat,Sheridan, Thomas,Yayla, Hatice G.
supporting information, p. 2766 - 2770 (2020/05/18)
C–F functionalization of arenes with a range of alcohol and pyrazole nucleophiles has been achieved without the need for metal catalysts or highly electron-poor substrates. Treatment of fluoroarenes with alcohols or pyrazoles and DDQ under irradiation by blue LED light provides the corresponding substituted products. The procedure is complementary to classical SNAr chemistry which generally requires basic reaction conditions and high temperatures, and provides products under non-basic conditions at ≈ 40 °C.
Regioselective Halogenation of Arenes and Heterocycles in Hexafluoroisopropanol
Tang, Ren-Jin,Milcent, Thierry,Crousse, Benoit
, p. 930 - 938 (2018/01/28)
Regioselective halogenation of arenes and heterocycles with N-halosuccinimides in fluorinated alcohols is disclosed. Under mild condition reactions, a wide diversity of halogenated arenes are obtained in good yields with high regioselectivity. Additionally, the versatility of the method is demonstrated by the development of one-pot sequential halogenation and halogenation-Suzuki cross-coupling reactions.
List fluoro Radicamine compounds and their use and preparation method
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Paragraph 0082; 0083; 0085, (2017/12/02)
The invention discloses a mono-fluorinated Radicamine compound which has a structure as shown in a formula (1), and further provides a preparation method for the mono-fluorinated Radicamine compound with the structure as shown in the formula (1) and an application of the mono-fluorinated Radicamine compound or the mono-fluorinated Radicamine compound prepared with the method to preparation of drugs for preventing and/or treating diabetes, drugs for preventing and/or treating Gaucher's diseases, drugs for preventing and/or treating tumors or antiviral drugs. The mono-fluorinated Radicamine compound provided by the invention is good in glycosidase inhibition activity.
Fluorinated Radicamine A and B: Synthesis and Glycosidase Inhibition
Li, Yi-Xian,Iwaki, Ren,Kato, Atsushi,Jia, Yue-Mei,Fleet, George W. J.,Zhao, Xuan,Xiao, Min,Yu, Chu-Yi
, p. 1429 - 1438 (2016/03/16)
Fluorinated derivatives of radicamine A and radicamine B have been synthesized from D-arabinose-derived cyclic nitrone. Structure-activity relationship studies showed that glycosidase inhibition of these fluorinated derivatives was significantly influenced by the position of the fluorine atom. C-7 or C-11 fluorination of the aromatic ring decreased α-glucosidase inhibition of the derivatives, whereas C-8 or C-10 fluorination preserved glycosidase inhibitory activities. Fluorinated derivatives of radicamine A and B have been synthesized from D-arabinose-derived cyclic nitrone. Structure-activity relationship studies revealed that glycosidase inhibition of these fluorinated derivatives was significantly influenced by the position of the fluorine atom.
GLUCOSYLCERAMIDE SYNTHASE INHIBITORS FOR THE TREATMENT OF DISEASES
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Paragraph 000274, (2015/04/15)
Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions associated with the enzyme glucosylceramide synthase (GCS).
New oxabispidine compounds for the treatment of cardiac arrhythmias
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Page/Page column 58, (2008/06/13)
There is provided compounds of formula I, wherein R1, R2, R3, R41 to R46, X, Y and Z have meanings given in the description, which compounds are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias.
PROCESS FOR THE PREPARATION OF N,N′- DISUBSTITUTED OXABISPIDINES
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Page/Page column 33, (2010/11/25)
There is provided a process for the preparation of a sulfonic acid salt of formula I, or a solvate thereof, which process comprises hydrogenating a sulfonic acid salt of formula II,. or a solvate thereof; in the presence of a solvent system consisting essentially of water, a C3-5 secondary alkyl alcohol and no more than 15% v/v of another organic solvent, wherein the sulfonic acid salt of formula I is optionally, without isolation, converted to a compound of formula IX, or a pharmaceutically-acceptable derivative thereof, wherein R1, R2, R3, R6, R7, R8, A, B and D have meanings given in the description.
NOVEL OXABISPIDINE COMPOUNDS AND THEIR USE IN THE TREATMENT OF CARDIAC ARRHYTHMIAS
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Page/Page column 85, (2008/06/13)
There is provided compounds of formula (I), wherein R1, R2, R3, R4, R 41 to R46, A, B and G have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias.
Nonpeptide αvβ3 Antagonists. 8. In Vitro and in Vivo Evaluation of a Potent αvβ3 Antagonist for the Prevention and Treatment of Osteoporosis
Hutchinson, John H.,Halczenko, Wasyl,Brashear, Karen M.,Breslin, Michael J.,Coleman, Paul J.,Duong, Le T.,Fernandez-Metzler, Carmen,Gentile, Michael A.,Fisher, John E.,Hartman, George D.,Huff, Joel R.,Kimmel, Donald B.,Leu, Chih-Tai,Meissner, Robert S.,Merkle, Kara,Nagy, Rose,Pennypacker, Brenda,Perkins, James J.,Prueksaritanont, Thomayant,Rodan, Gideon A.,Varga, Sandor L.,Wesolowski, Greg A.,Zartman, Amy E.,Rodan, Sevgi B.,Duggan, Mark E.
, p. 4790 - 4798 (2007/10/03)
3(S)-(6-Methoxypyridin-3-yl)-3-{2-oxo-3-[3-(5,6,7,8-tetrahydro-[1,8] -naphthyridin-2-yl)propyl]-imidazolidin-1-yl}propionic acid 6 was identified as a potent and selective antagonist of the αvβ3 receptor. This compound has an excellent in vitro profile (IC50 = 0.08 nM), a significant unbound fraction in human plasma (12%), and good pharmacokinetics in rat, dog, and rhesus monkey. On the basis of the efficacy shown in three in vivo models of bone turnover, the compound was selected for clinical development. To support the ongoing metabolism and safety studies, a novel strategy was employed in which a series of oxidized derivatives of 6 were prepared by exposure of 6 (or the methyl ester) to chemical oxidizing agents. These products proved useful in the identification of active metabolites generated by either in vitro or in vivo metabolism.
