- Mild regioselective iodination of pyrazoles using n-butyltriphenylphosphonium peroxodisulfate
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A practical, efficient and inexpensive method of synthesis of iodopyrazoles by the reaction of pyrazoles with iodine using n-butyltriphenylphosphonium peroxodisulfate as an oxidant at room temperature is reported. The use of n-butyltriphenylphosphonium peroxodisulfate is feasible due to its easy preparation and handling, high stability and activity.
- Gorjizadeh,Afshari,Naseh
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- MANUFACTURING METHOD OF AROMATIC IODINE COMPOUND USING DISULFIDE AS CATALYST
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To manufacture an aromatic iodine compound under a mild condition at low cost and high yield.SOLUTION: There is provided a manufacturing method of an aromatic iodine compound by reacting an aromatic compound and an iodination agent in a presence of a cata
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Paragraph 0020
(2020/04/04)
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- TEMPO-mediated C-H amination of benzoxazoles with N-heterocycles
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The direct amination of benzoxazoles at C2 using N-heterocycles as nitrogen sources has been developed for the first time. Several kinds of inexpensive oxidants and also electricity were effective for this transformation in the presence of 2,2,6,6- tetram
- Liu, Qiang,Yu, Xiao-Qi,Wang, Jian,Li, Jiang-Hua,Guo, Yidong,Dong, Hongbo
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p. 12797 - 12803
(2020/11/09)
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- Disulfide-Catalyzed Iodination of Electron-Rich Aromatic Compounds
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Herein, a disulfide-catalyzed electrophilic iodination of aromatic compounds using 1,3-diiodo-5,5-dimethylhydantoin (DIH) has been developed. The disulfide activates DIH as a Lewis base to promote the iodination reaction in acetonitrile under mild conditions. This system is applicable to a wide range of electron-rich aromatic compounds, including acetanilide, anisole, imidazole, and pyrazole derivatives.
- Iida, Keisuke,Ishida, Shunsuke,Watanabe, Takamichi,Arai, Takayoshi
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- Disulfide-Catalyzed Iodination of Electron-Rich Aromatic Compounds
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Herein, a disulfide-catalyzed electrophilic iodination of aromatic compounds using 1,3-diiodo-5,5-dimethylhydantoin (DIH) has been developed. The disulfide activates DIH as a Lewis base to promote the iodination reaction in acetonitrile under mild conditions. This system is applicable to a wide range of electron-rich aromatic compounds, including acetanilide, anisole, imidazole, and pyrazole derivatives.
- Iida, Keisuke,Ishida, Shunsuke,Watanabe, Takamichi,Arai, Takayoshi
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p. 7411 - 7417
(2019/06/18)
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- Photocatalytic Oxidative Iodination of Electron-Rich Arenes
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A visible-light-mediated oxidative iodination of electron-rich arenes has been developed. 2.5 mol% of unsubstituted anthraquinone as photocatalyst were used in combination with elementary iodine, trifluoroacetic acid and oxygen as the terminal oxidant. The iodination proceeds upon irradiation in non- or weakly-electron donating solvents (DCM, DCE and benzene) wherein a spectral window in strongly coloured iodine solutions can be observed at around 400 nm. The method provides good to excellent yields (up to 98%) and shows excellent regioselectivity and good functional group tolerance (triple bonds, ketone, ester, amide). Moreover, the photo-iodination was also upscaled to a 5 mmol scale (1.1 g). Mechanistic investigations by intermediate trapping and competition experiments indicate a photocatalytic arene oxidation and the subsequent reaction with iodine as a likely mechanistic pathway. (Figure presented.).
- Narobe, Rok,Düsel, Simon J. S.,Iskra, Jernej,K?nig, Burkhard
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supporting information
p. 3998 - 4004
(2019/07/17)
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- Transition-Metal-Free Selective Iodoarylation of Pyrazoles via Heterocyclic Aryliodonium Ylides
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A one-pot transition-metal-free selective iodoarylation of pyrazoles with aryliodine diacetates has been developed. The reaction proceeds via the generation of NH-pyrazole-iodonium salts in situ, followed by sequential phen/K2CO3-mediated intermolecular arylation. When the iodonium ylide was directly used as substrate, the difunctionalization products could be prepared in high yield under base- and metal-free conditions. This transformation provides an efficient route to high-value multisubstituted pyrazole derivatives from simple and readily available substrates.
- Lu, Nannan,Huang, Liangsen,Xie, Lili,Cheng, Jiajia
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p. 3437 - 3443
(2018/07/29)
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- HETEROARYL COMPOUNDS AND PHARMACEUTICAL APPLICATIONS THEREOF
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The present invention provides herein is a heteroaryl compound or a stereoisomer, a geometric isomer, a tautomer, a racemate, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, as well as a pharmaceutical composition containing the compound disclosed herein. The present invention also provides herein is use of the compound or the pharmaceutical composition thereof disclosed herein in the manufacture of a medicine for treating autoimmune diseases or proliferative diseases.
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Paragraph 00689
(2016/01/25)
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- THERAPEUTIC COMPOUNDS AND USES THEREOF
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The present invention relates to compounds of formula (I): and to salts thereof, wherein A has any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.
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Page/Page column 153
(2016/05/02)
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- Copper-catalyzed arylation of nitrogen heterocycles from anilines under ligand-free conditions
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The arylation of pyrazole and derivatives can be achieved by coupling arenediazonium species (formed in situ from anilines) by using a catalytic system that employs low-toxicity and inexpensive copper metal under very mild and ligand-free conditions (T = 20 ° C). From other nitrogen heterocycles, the presence of an additive (NBu4I) significantly improves the efficiency of the catalytic system. These results represent the first examples of C-N bond formation from arenediazonium species.
- Toummini, Dounia,Tlili, Anis,Bergs, Julien,Ouazzani, Fouad,Taillefer, Marc
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supporting information
p. 14619 - 14623
(2015/01/09)
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- Green iodination of pyrazoles with iodine/hydrogen peroxide in water
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In this Letter, we describe a practical, green iodination of pyrazoles to form the corresponding 4-iodopyrazole derivatives. The reaction takes place in water, using only 0.5 equiv of iodine and 0.6 equiv of hydrogen peroxide, a system that generates water as the only reaction by-product.
- Kim, Mary M.,Ruck, Rebecca T.,Zhao, Dalian,Huffman, Mark A.
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p. 4026 - 4028
(2008/09/20)
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- A fast and efficient bromination of isoxazoles and pyrazoles by microwave irradiation
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A fast and efficient method has been developed for the bromination of isoxazoles and pyrazoles using microwave irradiation. In this method, N-bromosuccinimide was used in different acid solvents according to the reactivity of the substrates to give mono-b
- Li, Guo,Kakarla, Ramesh,Gerritz, Samuel W.
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p. 4595 - 4599
(2008/02/06)
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- SYNTHESIS AND REACTION OF TRIBUTYLSTANNYLPYRAZOLES
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1,3-Dipolar cycloaddition reaction of diazomethane and ethyl diazoacetate with tributylstannylacetylenes occurred regioselectively to afford the corresponding 3(5)-tributylstannylpyrazoles.The cycloaddition reaction of 3-phenylsydnone with the stannylacetylenes proceeded also regioselectively, and 3-tributylstannyl-1-phenylpyrazoles were isolated. 4-Tributylstannyl- and 5-tributylstannyl-1-phenylpyrazole were prepared by the stannylation of 4-lithio- and 5-lithio-1-phenylpyrazoles with tributylstannyl chloride.Iodination, benzoylation, and phenylation of the stannylpyrazoles were examined.
- Sakamoto, Takao,Shiga, Futoshi,Uchiyama, Daishi,Kondo, Yoshinori,Yamanaka, Hiroshi
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p. 813 - 818
(2007/10/02)
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