133228-21-4Relevant articles and documents
Sequential SNAr Reaction/Suzuki-Miyaura Coupling/C-H Direct Arylations Approach for the Rapid Synthesis of Tetraaryl-Substituted Pyrazoles
Morita, Taiki,Kobayashi, Daisuke,Matsumura, Keisuke,Johmoto, Kohei,Uekusa, Hidehiro,Fuse, Shinichiro,Takahashi, Takashi
supporting information, p. 1626 - 1630 (2015/08/06)
A rapid synthesis of 1,3,4,5-tetraaryl-substituted pyrazoles has been achieved through a sequence of SNAr reaction/Suzuki-Miyaura coupling/Pd-catalyzed direct arylations that used 3-iodo-1H-pyrazole as a scaffold. Pyrazoles with four different aryl groups were synthesized in a straightforward manner with no extra synthetic steps, such as protection/deprotection or the introduction of activating/directing groups, using readily available substrates and reagents. The developed synthetic approach enabled the structurally diverse synthesis of multiaryl-substituted pyrazoles without using a glovebox technique.
THIAZOLOPYRIMIDINONES AS MODULATORS OF NMDA RECEPTOR ACTIVITY
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Paragraph 0498, (2015/04/28)
The present invention relates to certain thiazolopyrimidinone compounds for use in modulating NMDA receptor activity, pharmaceutical compositions comprising such compounds and methods of treating neurological and psychiatric conditions.
Selective palladium-catalyzed direct C-H arylation of unsubstituted N-protected pyrazoles
Kumpulainen, Esa T. T.,Pohjakallio, Antti
supporting information, p. 1555 - 1561 (2014/06/09)
A highly selective C-5 arylation of N-dimethylaminosulfamoyl-protected pyrazole with aryl bromides is catalyzed by 2-5 mol% palladium in the presence of triphenylphosphine ligand and carboxylic acid additive. Selectivities up to 45:1 (C-5:C-4) can be achieved by running the reaction in non-polar solvents. A thorough study of scope and limitations shows good general tolerance of aryl bromide substitution. However, limitations on tolerance of ortho-subsitution and protic functional groups were established. Together with a telescoped deprotection step this method presents a viable alternative for the synthesis of C-3 arylated pyrazole building blocks.
HETEROCYCLIC COMPOUND
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Paragraph 0581, (2015/01/18)
The present invention provides an agent for the prophylaxis or treatment of autoimmune diseases (e.g., psoriasis, rheumatoid arthritis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus etc.) and the like, which has a superior Tyk2 inhibitory action. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
HETEROCYCLIC COMPOUND
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Page/Page column 53, (2013/02/28)
Provided is a compound useful for the prophylaxis or treatment of cancer. The present invention relates to a compound represented by formula (I): wherein each symbol in the formula is as defined in the specification, or a salt thereof or a prodrug thereof, which is useful for the prophylaxis or treatment of cancer.
THIENOPYRIMIDINE AS CDC7 KINASE INHIBITORS
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Page/Page column 209-210, (2010/09/18)
The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, or a prodrug thereof, which is useful for the prophylaxis or treatment of cancer
METHYL SULFANYL PYRMIDMES USEFUL AS ANTIINFLAMMATORIES, ANALGESICS, AND ANTIEPILEPTICS
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Page/Page column 183-184, (2010/12/18)
The present invention relates to pyrimidine derivatives of Formula (Ia) and (Ib) (including tautomers, isomers, prodrugs, and pharmaceutically acceptable salts thereof). Said compounds are useful in the treatment of pain (such as neuropathic pain), inflammation, and epilepsy (by acting as anticonvulsants). Methods of medical treatment making use of said compounds, as well as additional compounds of Formula (IIa) and (IIb), are also disclosed.
FUNGICIDAL MIXTURES
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Page/Page column 87, (2008/12/07)
Disclosed is a fungicidal composition comprising (a) at least one compound selected from the compounds of Formula 1 N-oxides, and salts thereof, insert Formula 1 here wherein R1, R2, A, G, Q, W1, W2, X and n are otherwise as defined in the disclosure, and (b) at least one additional fungicidal compound. Also disclosed is a method for controlling plant diseases caused by fungal plant pathogens comprising applying to the plant or portion thereof, or to the plant seed, a fungicidally effective amount of the aforesaid composition.
HETEROCYCLIC HYDRAZIDE COMPOUND AND PESTICIDAL USE OF THE SAME
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Page/Page column 389-390, (2008/12/08)
A hydrazide compound represented by the formula (I), an N-oxide thereof or suitable salt thereof: has excellent pesticidal activity.
HYDRAZIDE COMPOUND AND PESTICIDAL USE OF THE SAME
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Page/Page column 487, (2008/06/13)
A hydrazide compound represented by the formula (1): has excellent pesticidal activity.