90534-62-6Relevant academic research and scientific papers
A novel and green synthesis of indolone-N-amino acid derivatives via the Passerini three-component reactions in water
Li, Rong-Kun,Yang, Quan-Li,Liu, Yi,Li, Dong-Wei,Huang, Nian-Yu,Liu, Ming-Guo
, p. 345 - 348 (2016)
A green Passerini three-component reaction of 2-(4-oxo-4,5,6,7-tetrahydro-1H-indol-1-yl)acetic acid with alkyl or aryl isocyanides and aldehydes was reported under aqueous conditions at 35 °C for 1 h, and 21 indolone-N-amino acid derivatives were prepared
Copper-Nitrene-Catalyzed Desymmetric Oxaziridination/1,2-Alkyl Rearrangement of 1,3-Diketones toward Bicyclic Lactams
Han, Xue,Shan, Li-Xin,Tu, Yong-Qiang,Wang, Hong,Yang, Ming,Zhang, Chang-Sheng,Zhang, Fu-Min,Zhang, Wen-Shuo,Zhang, Xiao-Ming,Zhu, Jin-Xin
supporting information, p. 22688 - 22692 (2021/09/18)
Although copper-nitrene has been extensively studied as a versatile active species in various transformations, asymmetric reactions involving copper-nitrene have been limited to the aziridination of olefins. Herein, we report the novel copper-nitrene-catalyzed desymmetric oxaziridination reaction of cyclic diketones with alkyl azides and the subsequent rearrangement of the resulting highly active intermediate, which produces a synthetically challenging chiral bicyclic lactam containing a quaternary carbon center. This procedure not only enriches the copper-nitrene-catalyzed asymmetric reactions, but also provides an alternative strategy to address the inherent challenges of catalytic asymmetric Schmidt reactions. This unique reaction could inspire the investigation of novel copper-nitrene-catalyzed asymmetric transformations and their reaction mechanisms.
Urea decomposition: Efficient synthesis of pyrroles using the deep eutectic solvent choline chloride/urea
Hu, Lanfang,Luo, Juan,Lu, Dan,Tang, Qiang
supporting information, p. 1698 - 1701 (2018/04/02)
A simple and efficient method is reported for the synthesis of pyrroles via condensation of a series of tricarbonyl compounds with ammonia, which was generated in situ from decomposition of the deep eutectic solvent choline chloride/urea.
Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of sulphone-based CRTh2 antagonists
Buil, Maria Antonia,Calbet, Marta,Castillo, Marcos,Castro, Jordi,Esteve, Cristina,Ferrer, Manel,Forns, Pilar,González, Jacob,López, Sara,Roberts, Richard S.,Sevilla, Sara,Vidal, Bernat,Vidal, Laura,Vilaseca, Pere
, p. 102 - 133 (2016/03/04)
Monocyclic and bicyclic ring systems were investigated as the "core" section of a series of diphenylsulphone-containing acetic acid CRTh2 receptor antagonists. A range of potencies were observed and single-digit nanomolar potencies were obtained in both the monocyclic and bicyclic cores. Residence times for the monocyclic compounds were very short. Some of the bicyclic cores displayed better residence times. A methyl group in the northern part of the core, between the head and tail was a necessary requirement for the beginnings of long residence times. Variations of the tail substitution maximised potencies and residence times.
Understanding the Scope of Feist–Bénary Furan Synthesis: Chemoselectivity and Diastereoselectivity of the Reaction Between α-Halo Ketones and β-Dicarbonyl Compounds
Peng, Yi,Luo, Juan,Feng, Qiang,Tang, Qiang
, p. 5169 - 5179 (2016/10/26)
Feist–Bénary furan synthesis, the reaction between α-halocarbonyl and β-dicarbonyl compounds, has been known as an efficient method for generating many different types of furans containing a carbonyl group at C-3. However, it has also been reported that, under similar reaction conditions, intermediate tricarbonyl species could be further converted to alternative furan isomers through the application of a Paal–Knorr synthesis. In this manuscript, we investigate the chemoselectivity and diastereoselectivity of furan synthesis from α-halo ketones and β-dicarbonyl compounds, by carrying out the separation and characterization of the intermediates involved in the reaction. Additionally, a one-pot Feist–Bénary furan synthesis from α-halo ketones and β-dicarbonyl compounds without any base or solvent has also been developed.
HYDROXAMATE DERIVATIVES FOR HDAC INHIBITOR, AND THE PHARMACEUTICAL COMPOSITION COMPRISING THEREOF
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Paragraph 0770-0772, (2014/10/29)
The present invention relates to a novel hydroxamate derivatives, more specifically, to novel hydroxamate derivatives having inhibitory activity against Histone Deacetylase (HDAC), isomers thereof, pharmaceutically acceptable salts thereof, hydrates or solvates thereof, use for preparing pharmaceutical compositions, pharmaceutical compositions comprising the same, treatment method using said composition, and a preparing method of novel hydroxamate derivatives. The novel selective hydroxamate derivatives having inhibitory activity against Histone Deacetylase (HDAC) compositions can be used for treatment of inflammatory disease, rheumatoid arthritis, or degenerative disease.
HYDROXAMATE DERIVATIVES FOR HDAC INHIBITOR, AND THE PHARMACEUTICAL COMPOSITION COMPRISING THEREOF
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Page/Page column 165; 166, (2013/05/21)
The present invention relates to a novel hydroxamate derivatives, more specifically, to novel hydroxamate derivatives having inhibitory activity against Histone Deacetylase (HDAC), isomers thereof, pharmaceutically acceptable salts thereof, hydrates or solvates thereof, use for preparing pharmaceutical compositions, pharmaceutical compositions comprising the same, treatment method using said composition, and a preparing method of novel hydroxamate derivatives. The novel selective hydroxamate derivatives having inhibitory activity against Histone Deacetylase (HDAC) compositions can be used for treatment of inflammatory disease, rheumatoid arthritis, or degenerative disease.
NOVEL ORGANIC COMPOUND AND ORGANIC LIGHT-EMITTING DEVICE INCLUDING THE SAME
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Page/Page column 22-23, (2012/02/01)
The present invention provides a blue or green phosphorescent organic electroluminescent device which has high luminous efficiency. An organic electroluminescent device includes a light-emitting layer containing a pyrroloindole compound represented by gen
Development of scalable manufacturing routes to AZD1981. Application of the Semmler-Wolff aromatisation for synthesis of the indole-4-amide Core
Sulur, Manjunatha,Sharma, Parhalad,Ramakrishnan, Ravi,Naidu, Ravi,Merifield, Eric,Gill, Duncan M.,Clarke, Adrian M.,Thomson, Colin,Butters, Michael,Bachu, Sreekanth,Benison, Colin H.,Dokka, Nagaraju,Fong, Emily R.,Hose, David R. J.,Howell, Gareth P.,Mobberley, Siobhan E.,Morton, Simon C.,Mullen, Alexander K.,Rapai, Jayan,Tejas, Bharathi
, p. 1746 - 1753 (2013/01/15)
A safe and efficient synthesis of AZD1981 is described in which the indole 4-amide core is formed by a Semmler-Wolff aromatisation of a cyclohexenone oxime fused to a pyrrole ring. The substrate was obtained via Paal-Knorr pyrrole synthesis, followed by i
INTERMEDIATES AND PROCESSES FOR THE PREPARATION OF 4- (ACETYLAMINO) ) -3- [ (4-CHLORO-PHENYL) THIO] -2-METHYL-1H-INDOLE-1-ACETIC ACID
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Page/Page column 23-24, (2011/02/24)
The invention relates to compounds of formula (X), and salts thereof, and their use as intermediates in improved manufacturing processes for the synthesis of pharmaceutical compound of formula (I): X is =0, =N-0H or =N-OC(O)Me; Y is hydrogen, PhS- or p-ch
