- Synthesis method of 2-halo-5-bromobenzoic acid
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The invention discloses a synthesis method of 2-halo-5-bromobenzoic acid. The method comprises the following steps of under the action of sulfuric acid, carrying out a bromination reaction on o-halo-benzoic acid and NBS in an organic solvent, and after the reaction is finished, carrying out posttreatment to obtain 2-halo-5-bromobenzoic acid. The method has the advantages of being short in reactionroute, simple in operation, environmentally friendly, safe and economical and has a broad application prospect.
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Paragraph 0038-0042
(2019/10/01)
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- Preparation method of 2,5-dihalo-benzoic acid
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The invention discloses a preparation method of 2,5-dihalo-benzoic acid. The method comprises the following steps: concentrated sulfuric acid is added dropwise to a mixed solution containing sodium bromide, periodate and 2-halo-benzoic acid in presence of water and acetic acid, the mixed solution is subjected to a reaction, and 2,5-dihalo-benzoic acid is prepared. The problems of long time neededfor preparation, high reaction temperature and the like of the preparation method of 2,5-dihalo-benzoic acid in the prior art can be solved.
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Paragraph 0035-0037
(2018/05/16)
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- TRIAZOLONES DERIVATIVES FOR USE IN THE TREATMENT, AMELIORATION OR PREVENTION OF A VIRAL DISEASE
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The present invention relates to a compound having the general formula (I), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, prodrug, tautomer, racemate, codrug, cocrystal, enantiomer, or diastereomer or mixture thereof, which is useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
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Page/Page column 54
(2017/04/18)
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- INHIBITORS OF STEAROYL-COA DESATURASE
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Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity.
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- Synthesis and structural characterization of new phosphinooxazoline complexes of iron
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The first phosphinooxazoline chelate complexes of iron were synthesized, and their structural and electronic properties were studied. The known phosphinooxazolines 2-(2-(diphenylphosphino)phenyl)-4,5-dihydrooxazole (7a), 2-(2-(diphenylphosphino)phenyl)-4,
- Sedinkin, Sergey L.,Rath, Nigam P.,Bauer, Eike B.
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p. 3081 - 3091
(2008/12/22)
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- Design, synthesis, and pharmacological evaluation of N-bicyclo-5-chloro-1H-indole-2-carboxamide derivatives as potent glycogen phosphorylase inhibitors
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As a result of the various N-bicyclo-5-chloro-1H-indole-2-carboxamide derivatives with a hydroxy moiety synthesized in an effort to discover novel glycogen phosphorylase (GP) inhibitors, 5-chloro-N-(5-hydroxy-5,6,7,8-tetrahydronaphthalen-2-yl)-1H-indole-2
- Onda, Kenichi,Shiraki, Ryota,Ogiyama, Takashi,Yokoyama, Kazuhiro,Momose, Kazuhiro,Katayama, Naoko,Orita, Masaya,Yamaguchi, Tomohiko,Furutani, Masako,Hamada, Noritaka,Takeuchi, Makoto,Okada, Minoru,Ohta, Mitsuaki,Tsukamoto, Shin-ichi
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experimental part
p. 10001 - 10012
(2009/04/06)
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- Synthesis and SAR of indazole-pyridine based protein kinase B/Akt inhibitors
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A series of heteroaryl-pyridine containing inhibitors of Akt are reported. The synthesis and structure-activity relationships are discussed, leading to the discovery of a indazole-pyridine analogue (Ki = 0.16 nM). These compounds bind in the ATP binding site, are potent, ATP competitive, and reversible inhibitors of Akt activity. No selectivity amongst the Akt isoforms is observed for this analogue, but there is good selectivity against an panel of other kinases. It is least selective for other members of the AGC family of kinases but is nonetheless 40-fold selective for Akt over PKA. The compound shows cellular activity and significantly slows tumor growth in vivo.
- Woods, Keith W.,Fischer, John P.,Claiborne, Akiyo,Li, Tongmei,Thomas, Sheela A.,Zhu, Gui-Dong,Diebold, Robert B.,Liu, Xuesong,Shi, Yan,Klinghofer, Vered,Han, Edward K.,Guan, Ran,Magnone, Shayna R.,Johnson, Eric F.,Bouska, Jennifer J.,Olson, Amanda M.,Jong, Ron de,Oltersdorf, Tilman,Luo, Yan,Rosenberg, Saul H.,Giranda, Vincent L.,Li, Qun
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p. 6832 - 6846
(2007/10/03)
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- Kinase inhibitors
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Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are compositions which inhibit protein kinases and methods of inhibiting protein kinases in a patient.
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- Kinase inhibitors
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Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are compositions which inhibit protein kinases and methods of inhibiting protein kinases in a patient.
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Page/Page column 39
(2010/01/31)
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- Regioselective ortho-lithiation of chloro and bromo substituted fluoroarenes
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Deprotonation of fluoroarenes carrying chlorine or bromine as additional substituents occurs always at a fluorine adjacent position if accomplished with potassium tert-butoxide activated butyllithium or lithium 2,2,6,6-tetramethylpiperidide.
- Mongin, Florence,Schlosser, Manfred
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p. 6551 - 6554
(2007/10/03)
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- Fluorine as an ortho-directing group in aromatic metalation: Generality of the reaction and the high position of fluorine in the Dir-Met potency scale
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Many para-substituted fluorobenzenes can be lithiated ortho to fluorine in moderate to good yields, often with one of the dialkylamide bases, lithium diisopropylamide (LDA) or lithium 2,2,6,6-tetramethylpiperidide (LiTMP). Intramolecular competition experiments reveal that fluorine is one of the most potent Dir-Met activating groups under these conditions.
- Bridges,Lee,Maduakor,Schwartz
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p. 7495 - 7498
(2007/10/02)
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