93501-84-9Relevant academic research and scientific papers
COMPOUNDS FOR USE IN THE TREATMENT OF LIVER DISEASE
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Paragraph 00129-00130; 00135, (2021/02/26)
Bile acid derivatives, methods of manufacture thereof, and uses thereof are disclosed herein. The bile acid derivatives have demonstrated potential as therapeutics for treating liver disease.
One-pot four-component tandem synthesis of novel sulfonamide-1, 2, 3-triazoles catalyzed by reusable copper (II)-adsorbed on mesoporous silica under ultrasound irradiation
Talha, Aicha,Mourhly, Asmae,Tachallait, Hamza,Driowya, Mohsine,El Hamidi, Adnane,Arshad, Suhana,Karrouchi, Khalid,Arsalane, Said,Bougrin, Khalid
, (2021/07/09)
A green and efficient synthesis of new sulfonamide-1,2,3-triazoles 5 in heterogeneous conditions has been developed. The procedure involved one-pot four-component tandem sulfonamidation/azidation/1,3-dipolar cycloaddition (1,3-DC) reactions under a cooperative effect of ultrasound irradiation and Cu (II) supported on amorphous mesoporous silica [mSiO2-Cu (II)] catalysis at room temperature in aqueous medium. In addition, the 1,4-disubstituted 1,2,3-triazoles 5 were synthesized by regioselective and chemoselective methods to afford the pure products in excellent yields and short reaction times under ultrasonic irradiation. The supported catalyst has been prepared from copper (II) nitrate by simple method using ultrasound activation and characterized by X-ray diffraction (XRD), Brunauer-Emmett-Teller (BET) method and Barrett-Joyner-Halenda (BJH) method. Also, the catalyst is easily prepared, stable, efficient, selective, and reusable under ultrasonic conditions.
Gold(I) Complexes Nuclearity in Constrained Ferrocenyl Diphosphines: Dramatic Effect in Gold-Catalyzed Enyne Cycloisomerization
Nguyen, Tuan-Anh,Roger, Julien,Nasrallah, Houssein,Rampazzi, Vincent,Fournier, Sophie,Cattey, Hélène,Sosa Carrizo, E. Daiann,Fleurat-Lessard, Paul,Devillers, Charles H.,Pirio, Nadine,Lucas, Dominique,Hierso, Jean-Cyrille
supporting information, p. 2879 - 2885 (2020/08/13)
Di-tert-butylated-bis(phosphino)ferrocene ligands bearing phosphino substituents R (R=phenyl, cyclohexyl, iso-propyl, mesityl, or furyl) allow tuning the selective formation of Au(I) halide complexes. Thus, dinuclear linear two-coordinate, but also rare mononuclear trigonal three-coordinate and tetrahedral four-coordinate complexes were formed upon tuning of the conditions. Both Au(I) chloride and rarer Au(I) iodide complexes were synthesized, and their X-ray diffraction analysis are reported. The significance of the control of structure and nuclearity in Au(I) complexes is further illustrated herein by its strong effect on the efficiency and selectivity of gold-catalysed cycloisomerization. Cationic linear digold(I) bis(dicyclohexylphosphino) ferrocenes outperform other catalysts in the demanding regioselective cycloisomerization of enyne sulphonamides into cyclohexadienes. Conversely, tetrahedral and trigonal cationic monogold(I) complexes were found incompetent for enyne cycloaddition. We used the two-coordinate linear electron-rich Au(I) complex 2 b (R=Cy) to extend the scope of selective intramolecular cycloaddition of different 1,6-enyne sulfonylamines with high activity and excellent selectivity to the endo cyclohexadiene products.
Ruthenium Carbene-Mediated Construction of Strained Allenes via the Enyne Cross-Metathesis/Cyclopropanation of 1,6-Enynes
Gao, Ming,Gao, Qiangqiang,Hao, Xiangbin,Wu, Ying,Zhang, Qingmin,Liu, Guohua,Liu, Rui
supporting information, p. 1139 - 1143 (2020/02/15)
Herein, we report on the unprecedented dimerization of 1,6-enynes using a commercially available ruthenium complex RuCl2(PPh3)3, which results in a series of bicyclo[3.1.0]hexyl allene derivatives in moderate to excellent yields. Mechanistic investigation indicates that the in-situ-generated ruthenium vinylidene undergoes a site-selective metathesis process to provide allenyl ruthenium carbene, which can be intramolecularly trapped by the pendent C=C bond of enyne through a [2 + 2] cycloaddition/metal elimination process.
Orthogonal Syntheses of 3.2.0 Bicycles from Enallenes Promoted by Visible Light
Serafino, Andrea,Balestri, Davide,Marchiò, Luciano,Malacria, Max,Derat, Etienne,Maestri, Giovanni
supporting information, p. 6354 - 6359 (2020/09/02)
Enallenes can be readily converted into two families of 3.2.0 (hetero)bicycles with high diastereoselectivities through the combination of visible light with a suitable Ir(III) complex (1 mol percent). Two complementary pathways, namely, a photocycloaddit
Cu(I)-catalyzed oxidative cyclization of enynamides: Regioselective access to cyclopentadiene frameworks and 2-aminofurans
Shen, Wen-Bo,Tang, Xiang-Ting,Zhang, Ting-Ting,Liu, Si-Yu,He, Jiang-Man,Su, Tong-Fu
supporting information, p. 6799 - 6804 (2020/09/15)
An efficient Cu(I)-catalyzed oxidative cyclization of alkynyl-tethered enynamides for the construction of fused bicyclic cyclopentadiene derivatives is disclosed. The cascade proceeds through alkyne oxidation, carbene/alkyne metathesis, and formal (3 + 2)
An unconventional sulfur-to-selenium-to-carbon radical transfer: Chemo-and regioselective cyclization of yne-ynamides
Dutta, Shubham,Prabagar,Vanjari, Rajeshwer,Gandon, Vincent,Sahoo, Akhila K.
supporting information, p. 1113 - 1118 (2020/03/11)
An uncommon sulfur → selenium → carbon radical transfer process is employed to develop an unprecedented selenyl radical-mediated regioselective cyclization of yne-tethered-ynamides. Density functional theory studies and HRMS experiments are used to establish a reactivity scale between thiyl and selenyl radicals. The unique features of this transformation include, (1) the chemoselective reactivity of RSe over RS, (2) regioselective RSe attack on alkyne over ynamide, (3) 5-exo-dig cyclization of yne-ynamide to unusual 4-selenyl-pyrroles, and (4) the green synthetic method. The reaction of methyldiselenide with yne-ynamides to methylselenopyrroles is also described.
3-HYDROXY-IMIDAZOLIDIN-4-ONE COMPOUNDS AS INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE
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Page/Page column 30-31, (2019/03/17)
The invention relates to a compound of Formula (I) : Formula (I), or pharmaceutically acceptable enantiomers, or salts thereof. The present invention also relates to the use of compounds of Formula (I) as selective inhibitors of indoleamine 2,3-dioxygenas
Gold-Catalyzed Annulations of N-Propargyl Ynamides with Anthranils with Two Distinct Chemoselectivities
Hsu, Yu-Chen,Hsieh, Shu-An,Liu, Rai-Shung
supporting information, p. 5288 - 5297 (2019/03/26)
Gold-catalyzed annulation of N-propargyl ynamides with anthranils can proceed by two distinct mechanisms. In the case of a terminal N-propargyl ynamide, its resulting α-imino gold carbene reacts with a tethered alkyne to generate a vinyl cation to enable hydrolysis, which ultimately yields a pyrrolo[2,3-b]quinoline derivative after treatment with p-toluenesulfonic acid. For an internal alkyne, its α-imino gold carbene reacts with a tethered alkyne via either a vinyl cation or an alkenylgold carbene; both paths ultimately lead to a 4-ketone-2-aminopyrrole derivative. Our mechanistic analysis indicates that water is a better nucleophile than anthranil for terminal ynamides, whereas water and anthranils are equally reactive for internal ynamides.
INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE
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Page/Page column 30, (2017/09/28)
The invention relates to a compound of Formula (I), or pharmaceutically acceptable enantiomers, or salts thereof. The present invention also relates to the use of compounds of Formula (I) as selective inhibitors of indoleamine 2,3-dioxygenase. The inventi
