- TRIAZOLONE COMPOUNDS AS mPGES-1 INHIBITORS
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The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
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Page/Page column 61; 62
(2014/01/08)
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- METALLIC AMIDOBORATES FOR FUNCTIONALIZING ORGANIC COMPOUNDS
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Metallic amidoborates, their anions and processing for making them are described which comprise at least one metallic cation or cationic complex and an anion comprising the moiety (R1)2N -B(R2)3, wherein each R1 independently represents Z1(Z1A)p-, wherein each Z1 and Z1A independently represents a carbon atom or a silicon atom and each p independently represents the integer 2 or 3 and each R2 independently represents a fluorine atom or Z2(Z2A)k -, wherein each Z2 independently represents a carbon atom, nitrogen atom or a silicon atom, each Z2A independently represents a hydrogen atom, a carbon atom or a silicon atom, and k represents a positive integer equal to the valence of Z2, wherein at least one of the R2 substituents is Z2(Z2A)k -. The metallic amidoborate compounds may be used to make metalated organic compounds, which in turn may be reacted with an electrophile to make organic compounds functionalized by the electrophile residue. The metallic amidoborate bases described herein are exceptionally stable, so that functionalization of the organic compound may be carried out rapidly and with high yield at room temperature.
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Page/Page column 25-27
(2012/07/13)
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- Palladium-catalyzed aryl amination-heck cyclization cascade: A one-flask approach to 3-substituted indoles
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(Chemical Equation Presented) Two for the price of one: A Pd/dppf-based catalyst provides access to the title compounds from 1,2-dihalogenated aromatic compounds and allylic amines in a single reaction flask. The initial aryl amination step occurs with excellent selectivity for the aryl iodide to ensure the formation of a single indole regioisomer, which can be functionalized in situ by N-arylation (see scheme). dba = dibenzylideneacetone, dppf = 1,1′-bis(diphenylphospanyl)ferrocene.
- Jensen, Thomas,Pedersen, Henrik,Bang-Andersen, Benny,Madsen, Robert,Jorgensen, Morten
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p. 888 - 890
(2008/09/20)
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- HCV NS3 PROTEASE INHIBITORS
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The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
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Page/Page column 54-55
(2008/12/05)
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- GLYCINE TRANSPORTER INHIBITOR
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The present invention provides a compound represented by the following formula or a pharmaceutically acceptable salt of the compound or a hydrate of the compound or the salt, which is useful for the prevention or treatment of diseases such as schizophreni
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Page/Page column 108-109
(2010/11/30)
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- Deprotonation of chloropyridines using lithium magnesates
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Chloropyridines are deprotonated using lithium magnesates. 4-Chloropyridine was deprotonated on treatment with 1/3 equiv of the highly coordinated magnesate Bu3(TMP)MgLi2 in THF at -10°C, as evidenced by trapping with I2. The use of Bu(TMP)2MgLi in Et 2O allowed the reaction of 2-chloropyridine, giving the 3-functionalized derivative as the main product. Mixtures of 3- and 4-functionalized derivatives were obtained when 2,6-dichloropyridine was involved in the reaction. Performing the reaction on 3-chloropyridine with lithium magnesates in THF, either the 4,4′-dimer or the 4-iodo derivative was formed after quenching by I2, the former using 1/3 equiv of Bu2(TMP)MgLi and the latter using 1 equiv of (TMP)3MgLi. Similar results were observed with 3,5-dichloropyridine, 2,5-dichloropyridine and 3-chloro-2-fluoropyridine. 1,2-Migration of the lithium arylmagnesate formed by deprotonation was proposed to justify the dimers formation.
- Awad, Ha?an,Mongin, Florence,Trécourt, Fran?ois,Quéguiner, Guy,Marsais, Francis
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p. 7873 - 7877
(2007/10/03)
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- Pyrazole derivatives
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The present invention relates to cis- and trans-forms of pyrazole derivatives, salts thereof, or agents containing the same, and represented by the general formula (I): wherein G represents a nitrogen containing saturated heterocyclic structure represented by the following formula: These compounds exhibit anti-tumor activity on 5-FU-resistant tumors and effects on P glycoprotein expressing, multiple-drug resistant tumors. An example of a pyrazole derivative which demonstrates 50% inhibition of tumor cell growth is 3-[4-(3-chloro-5-fluorophenyl)-1 piperazinyl]-1-[1-(3-chloro-2-pyridyl)-5-methyl-4-pyrazolyl)-1-trans-propene hydrochloride. Synthesis of the compounds represented by formula (I) can be prepared by any one of various routes such as a Mannich reaction, a Wittig reaction, reductive amination or substitution by allylation.
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- REGIOSELECTIVE ORTHO-LITHIATION OF HALOPYRIDINES. SYNTHESES OF ORTHO-DISUBSTITUTED PYRIDINES AND A CONVENIENT GENERATION OF 3,4-PYRIDYNE
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The regioselective ortho-lithiation of 3-chloro- (4), 3-fluoro- (7), 3-bromo- (10), 2-chloro- (22), and 4-chloropyridine (25) with lithium diisopropylamide affords, after quenching with various electrophiles, the corresponding ortho-disubstituted pyridine
- Gribble, Gordon W.,Saulnier, Mark G.
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p. 151 - 169
(2007/10/02)
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- Connection between metalation and cross-coupling strategies. A new convergent route to azacarbazoles
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New convergent synthesis of azacarbazoles through metalation, cross-coupling reaction and intramolecular substitution via (2-aminobenzene)boronic acid and ortho-fluoroiodopyridines.
- Rocca, Patrick,Marsais, Francis,Godard, Alain,Queguiner, Guy
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- Regioselective ortho lithiation of halopyridines
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Regioselective ortho lithiation of 2-, 3-, and 4-halopyridines is achieved with lithium diisopropylamide (-78°, tetrahydrofuran) to afford, upon quenching with electrophilic reagents, 2,3- and 3,4-disubstituted pyridines in good to excellent yield.
- Gribble, Gordon W.,Saulnier, Mark G.
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p. 4137 - 4140
(2007/10/02)
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