1576-14-3Relevant academic research and scientific papers
Kinase inhibitors (by machine translation)
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Paragraph 0539-0540, (2020/12/31)
The present invention relates to certain 4 - (substituted anilino) -2 - (substituted piperi -1 -yl) pyrimidine -5 - carboxamide compounds useful for the treatment or prevention of diseases or medical conditions mediated by signal transduction of CaMMK1 isotype. For example, such compounds and salts thereof may be used to treat or prevent a variety of different cancers. Diseases (including 2 diabetes) and/or immune-mediated diseases. (by machine translation)
Edaravone analogue as well as preparation method and application thereof
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Paragraph 0023-0024, (2020/03/16)
Edaravone analogue, preparation method thereof and application, compound according to the following structural formula: In-flight, R1 And R2 The compounds of the present invention are methyl, methoxy, ethyl, isopropyl, tert-butyl or sec-butyl . with GABAA receptor enhancing activity and radical scavenger activity, having neuroprotective action, and compounds of the present invention can be used as a stroke prevention and treatment drug.
A Propofol preparation method
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Paragraph 0027; 0028; 0029; 0030; 0031; 0032; 0033; 0034, (2017/10/28)
The invention provides a preparation method of propofol, which includes following steps: (1) performing Friedel-crafts reaction to p-nitrophenol and isopropanol or 2-halogenated propane under catalysis of an acid to prepare a compound I; (2) performing acylation protection to the compound I to prepare a compound II; (3) performing a reduction reaction to the compound II to prepare a compound III; (4) performing a diazo-reaction to the compound III to prepare a compound IV; and (5) under a weak reducing agent condition, performing a decomposition reaction to the compound IV and meanwhile carrying out hydrolysis under an alkaline condition to obtain the propofol V. The raw materials of the preparation method are easy to obtain. The preparation method is simple in process and is high in yield.
COMPOUNDS FOR USE IN THE TREATMENT OF PAIN
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Page/Page column 21, (2010/07/02)
The present invention concerns compounds derived from the anaethetic propofol. The compounds may be useful in the treatment of pain, particularly, but not exclusively, chronic pain and central pain sensitisation.
A convenient method for synthesizing modified 4-nitrophenols
Nakaike, Yumi,Kamijo, Yoshio,Mori, Satoshi,Tamura, Mina,Nishiwaki, Nagatoshi,Ariga, Masahiro
, p. 10169 - 10171 (2007/10/03)
β-Nitroenamine having a formyl group behaves as the synthetic equivalent of unstable nitromalonaldehyde upon treatment with ketones under basic conditions and leads to 2,6-disubstituted 4-nitrophenols. The present method is safer than the conventional one using sodium nitromalonaldehyde and enables the preparation of hitherto unknown nitrophenols.
Isotopic effect study of propofol deuteration on the metabolism, activity, and toxicity of the anesthetic
Helfenbein,Lartigue,Noirault,Azim,Legailliard,Galmier,Madelmont
, p. 5806 - 5808 (2007/10/03)
The use of isotopic substitution to delay the oxidative metabolism of the anesthetic propofol 1 was studied. The aromatic hydrogens of propofol 1 were replaced by deuterium to produce the mono- and trideuterated derivatives 4 and 5. In vitro metabolic stu
Propofol analogues. Synthesis, relationships between structure and affinity at GABA(A) receptor in rat brain, and differential electrophysiological profile at recombinant human GABA(A) receptors
Trapani, Giuseppe,Latrofa, Andrea,Franco, Massimo,Altomare, Cosimo,Sanna, Enrico,Usala, Marcello,Biggio, Giovanni,Liso, Gaetano
, p. 1846 - 1854 (2007/10/03)
A number of propofol (2,6-diisopropylphenol) congeners and derivatives were synthesized and their in a vitro capability to affect GABA(A) receptors determined by the inhibition of the specific [35S]-tert- butylbicyclophosphorothionate ([35S]TBPS) binding to rat whole brain membranes. Introduction of halogen (Cl, Br, and I) and benzoyl substituents in the para position of the phenyl group resulted in ligands with higher potency at inhibiting [35S]TBPS binding. A quantitative structure - affinity relationship (QSAR) study demonstrated that affinity is enhanced by increases in lipophilicity of the ligand whereas affinity is adversely affected by increases in size of the substituent para to the phenolic hydroxyl group. Consistent with the displacement of [35S]TBPS and with the activation of GABA(A) receptors, we demonstrate that ligands displaying high affinity (i.e., 2-4, and 8) are able to increase GABA-stimulated chloride currents in oocytes expressing human GABA(A) receptors and to directly activate chloride currents in an electrophysiological assay. Among them, compound 4 showed a rather peculiar profile in the electrophysiological examination with cloned α1β2γ2 GABA(A) receptors. Indeed, compared to propofol, it displayed a much greater efficacy at potentiating GABA-elicited chloride currents, but a much lower efficacy at producing a direct activation of the chloride channel in the absence of GABA. This behavior may give to compound 4 pharmacological properties that are more similar to anxiolytic and anticonvulsant drugs than to those of general anesthetics.
The synthesis and electrochemistry of CpTiCl2(OR) (R = alkyl, aryl) complexes
Fussing, Ingrid M. M.,Pletcher, Derek,Whitby, Richard J.
, p. 109 - 118 (2007/10/02)
The syntheses of several new CpTiCl2(OR) (R = alkyl, aryl) complexes are described.It was possible to isolate pure product when the R group is substituted such as to cause steric crowding at the metal centre; for example, particularly good yields of the p
Phenol transalkylation process
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, (2008/06/13)
Phenols having an unsubstituted ortho position are transalkylated in the ortho position by mixing them with an ortho-alpha-branched alkylphenol (e.g., 2,6-di-sec-butylphenol) and an aluminum phenoxide catalyst and heating the mixture to 100°-350°C., preferably in a closed system and in the presence of olefin corresponding in structure to the ortho-alpha-branched alkyl group.
