27088-84-2Relevant academic research and scientific papers
Syntheses and properties of donor - Acceptor-type 2,5-diarylthiophene and 2,5-diarylthiazole
Masui, Kentaro,Mori, Atsunori,Okano, Kunihiko,Takamura, Kenji,Kinoshita, Motoi,Ikeda, Tomiki
, p. 2011 - 2014 (2004)
Equation presented. Syntheses of differently substituted 2,5-diarylthiophenes and 2,5-diarylthiazoles are carried out with the palladium-catalyzed C-H substitution reaction using AgF as an activator. Remarkably strong photoluminescence is observed in 2,5-
Metal-Free Aerobic Oxidative Selective C-C Bond Cleavage in Heteroaryl-Containing Primary and Secondary Alcohols
Xia, Anjie,Qi, Xueyu,Mao, Xin,Wu, Xiaoai,Yang, Xin,Zhang, Rong,Xiang, Zhiyu,Lian, Zhong,Chen, Yingchun,Yang, Shengyong
, (2019/05/07)
A transition-metal-free aerobic oxidative selective C-C bond-cleavage reaction in primary and secondary heteroaryl alcohols is reported. This reaction was highly efficient and tolerated various heteroaryl alcohols, generating a carboxylic acid derivative and a neutral heteroaromatic compound. Experimental studies combined with density functional theory calculations revealed the mechanism underlying the selective C-C bond cleavage. This strategy also provides an alternative simple approach to carboxylation reaction.
Bicyclic alkaloid compound, preparation method and applications thereof
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, (2018/11/03)
The present invention relates to a bicyclic alkaloid compound, or a tautomer, a stereoisomer, a racemate, the non-equal mixture of enantiomers, a geometric isomer, a solvate, a pharmaceutically acceptable salt or a prodrug thereof, and a pharmaceutical composition containing the compound. The invention further discloses uses of the compounds and the pharmaceutical composition thereof as drugs, especially as anti-inflammatory drugs and anti-fibrotic drugs.
A new face of phenalenyl-based radicals in the transition metal-free C-H arylation of heteroarenes at room temperature: Trapping the radical initiator: Via C-C σ-bond formation
Ahmed, Jasimuddin,Sreejyothi,Vijaykumar, Gonela,Jose, Anex,Raj, Manthan,Mandal, Swadhin K.
, p. 7798 - 7806 (2017/10/30)
The radical-mediated transition metal-free approach for the direct C-H bond functionalization of arenes is considered as a cost effective alternative to transition metal-based catalysis. An organic ligand-based radical plays a key role by generating an aryl radical which undergoes a subsequent functionalization process. The design principle of the present study takes advantage of a relatively stable odd alternant hydrocarbon-based phenalenyl (PLY) radical. In this study, the first transition metal-free catalyzed direct C-H arylation of a variety of heteroarenes such as azoles, furan, thiophene and pyridine at room temperature has been reported using a phenalenyl-based radical without employing any photoactivation step. This protocol has been successfully applied to the gram scale synthesis of core moieties of bioactive molecules. The phenalenyl-based radical initiator has been characterized crystallographically by trapping it via the formation of a C-C σ-bond between the phenalenyl radical and solvent-based radical species.
Photon-Quantitative 6π-Electrocyclization of a Diarylbenzo[b]thiophene in Polar Medium
Li, Ruiji,Nakashima, Takuya,Galangau, Olivier,Iijima, Shunsuke,Kanazawa, Rui,Kawai, Tsuyoshi
supporting information, p. 1725 - 1730 (2015/08/06)
The high reactivity of 6π-electrocyclization in polar solvents has remained one of the important challenges for diarylethenes because of the emergence of a twisted intramolecular charge transfer (TICT) state at the excited state in such polar media, which usually quenches the photocyclization reaction. Herein we report on the preparation and highly efficient photocyclization of 2,3-diarylbenzo[b]thiophenes with nonsymmetric side-aryl units in a polar solvent. While the dithiazolylbenzo[b]thiophene showed a suppressed quantum yield of 6π-electrocyclization of 54% in methanol, the replacement of a thiazole unit with a thiophene ring led to a photon-quantitative 6π-cyclization reaction. The nonsymmetrical modification into the side-aryl units was considered to enhance the CH/π interactions between side-aryl units to support a photoreactive conformation in methanol. The stabilization of the photochromic reactive conformation is expected to suppress the formation of the TICT state at the excited state, leading to highly efficient photoreactivity.
NOVEL NUCLEOSIDE PHOSPHORAMIDATE COMPOUND AND USE THEREOF
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Paragraph 0083, (2015/11/24)
The present invention provides a novel nucleoside phosphoramidate compound, or a stereoisomer, salt, hydrate, solvate or crystal thereof for the treatment of Flaviviridae family viral infection, especially hepatitis C viral infection. The present invention also provides the pharmaceutical composition comprising a compound of the present invention, or a stereoisomer, salt, hydrate, solvate or crystal thereof and a use of the compound or the composition of the present invention in the treatment of Flaviviridae family viral infection, especially hepatitis C viral infection. The compound of the present invention has a good anti-HCV effect.
Programmed synthesis of arylthiazoles through sequential C-H couplings
Tani, Satoshi,Uehara, Takahiro N.,Yamaguchi, Junichiro,Itami, Kenichiro
, p. 123 - 135 (2014/01/06)
A programmed synthesis of privileged arylthiazoles via sequential C-H couplings catalyzed by palladium or nickel catalysts has been accomplished. This versatile protocol can supply all possible arylthiazole substitution patterns (2-aryl, 4-aryl, 5-aryl, 2
NITROGEN-CONTAINING AROMATIC HETEROCYCLYL COMPOUND
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Page/Page column 69, (2011/04/25)
The present invention provides a compound having excellent regulating action on blood lipid level. The present invention provides a compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, etc., wherein A represents a 5-membered nitrogen-containing aromatic heterocyclyl group; R1 represents COOH or the like; each R2 represents an alkyl or the like; each R3 represents an optionally substituted phenyl, an optionally substituted phenylalkyl, or the like; m represents 0, 1, 2, or 3; n represents 0 or 1; each of R4, R5, R6, and R7 represents H, an alkyl, or the like; and B represents an optionally substituted naphthyl, an optionally substituted aromatic heterocyclyl, or a group represented by the following formula (II) wherein each of B1 and B2 represents an optionally substituted phenyl or an optionally substituted aromatic heterocyclyl.
THIAZOLE AND OXAZOLE KINASE INHIBITORS
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Page/Page column 59-60, (2011/08/04)
The present invention is concerned with substituted azole derivatives that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant proteine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. In particular, several of these compounds are potent and selective Flt-3 inhibitors or/and syk inhibitors.
Cobalt-catalyzed C-SMe bond activation of heteroaromatic thioethers
Begouin, Jeanne-Marie,Rivard, Michael,Gosmini, Corinne
supporting information; experimental part, p. 5972 - 5974 (2010/11/02)
Cobalt-catalyzed activation of methylthio-substituted N-heterocycles facilitates either cross-coupling reactions with aryl- or benzylzinc compounds or synthesis of the corresponding zinc compounds.
