1481-32-9Relevant articles and documents
Functionalization of styrenes by copper-catalyzed borylation/ ortho-cyanation and silver-catalyzed annulation processes
Zhao, Wanxiang,Montgomery, John
, p. 12683 - 12686 (2015)
An efficient two-step method for the assembly of indanone derivatives starting from a simple vinyl arene has been developed. The sequence first involves addition of bis(pinacolato)diboron (B2pin2) and N-cyano-N-phenyl-p-methylbenzenesulfonamide (NCTS) to a broad range of styrenes by utilizing IMesCuCl as catalyst. This step simultaneously accomplishes hydroboration of the alkene and ortho cyanation of the benzene unit. The products thus obtained are further functionalized by a AgNO3/Selectfluor-mediated coupling of the BPin and cyano functionalities to annulate a new five-membered ring. This combined two-step sequence provides a versatile method for the site-selective derivatization of a broad range of vinyl arene substrates. A Cu and Ag sequence: The bis-functionalization of styrenes is accomplished through a copper-catalyzed process that enables hydroboration of the alkene and regioselective ortho cyanation of the arene. The resulting adducts are converted, by a radical cyclization process, into a cyclopentanone unit fused to the original aromatic ring. Together, these methods allow efficient cyclopentannulation of a broad range of styrene derivatives.
A concise synthesis of 2-benzoyl-1-indanones and 1-indanones from 2-aryl-1-tetralones
Kumari, Anusueya,Singh, Saurabh Kumar,Singh, Raj Bahadur,Bhunia, Sabyasachi,Ghosh, Partha
, p. 2313 - 2318 (2020/07/04)
Methyl-2-(3-oxo-3-aryl) benzoates derived from acid catalyzed air oxidative fragmentation of 2-aryl-1-tetralones were efficiently undergone intramolecular-Claisen condensation in the presence of potassium tertiary butoxide. The resulting 2-benzoyl-1-indanones formed in two-step ring contractions were further subjected to indium triflate mediated retro-Claisen condensation to get 1-indanones.
Synthesis and antitumor activity evaluation of 2-arylisoquinoline-1,3(2H, 4H)-diones in vitro and in vivo
Kang, Bo-Rui,Wang, Juan,Li, Huan,Li, Yan,Mei, Qi-Bing,Zhang, San-Qi
, p. 1340 - 1349 (2014/03/21)
Six 2-(2-acylaminobenzothiazol-6-yl)isoquinoline-1,3(2H,4H)-diones (1a-1f) and five 2-arylisoquinoline-1,3(2H,4H)-diones (1g-1k) were synthesized by refluxing homophthalic anhydrides with 2-acylaminobenzothiazolyl-6-amine or substituted aniline in glacial acetic acid. The cytotoxic activities of 1a-1k were evaluated via MTT method against A431, A549, and PC3. Compound 1b relatively displayed a higher cytotoxic activity than the others. The antitumor effect of 1b were evaluated in established nude mice PANC-1 xenograft model. The results suggest that compound 1b could potentially inhibit tumor growth.
Catalytic asymmetric cross-dehydrogenative coupling: Activation of C-H bonds by a cooperative bimetallic catalyst system
Cao, Weidi,Liu, Xiaohua,Peng, Ruixue,He, Peng,Lin, Lili,Feng, Xiaoming
, p. 3470 - 3472 (2013/05/23)
A cooperative bimetallic catalyst system was applied in the catalytic asymmetric cross-dehydrogenative coupling of β-ketoesters and xanthene. Various optically active xanthene derivatives bearing a quaternary stereogenic carbon center were obtained in moderate to good yields (up to 90%) with excellent enantioselectivities (up to 99% ee). Meanwhile, a transition-state model was proposed to explain the origin of the asymmetric induction.
Inter- and intramolecular hydroacylation of alkenes employing a bifunctional catalyst system
Vautravers, Nicolas R.,Regent, Damien D.,Breit, Bernhard
, p. 6635 - 6637 (2011/06/27)
Based on a conceptually innovative bifunctional P,N ligand, an efficient protocol for the rhodium-catalyzed inter- and intramolecular hydroacylation of alkenes has been developed.
SUBSTITUTED FLUOROETHYL UREAS AS ALPHA 2 ADRENERGIC AGENTS
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Page/Page column 18, (2008/12/04)
Therapeutic compounds, and methods, compositions, and medicaments related thereto are disclosed herein.
THERAPEUTIC FLUOROETHYLCYANO GUANIDINES
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Page/Page column 14, (2008/12/04)
Disclosed herein is compound having a formula as described herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
Synthesis of methylene-bridged analogues of biologically active pteridine derivatives
Slusarczyk, Magdalena,De Borggraeve, Wim M.,Toppet, Suzanne,Hoornaert, Georges J.
, p. 2987 - 2994 (2008/02/13)
The hepatitis C virus (HCV) is a major cause of liver disease worldwide. The HCV NS5B RNA-dependent RNA polymerase, which is a central enzyme in the replication of the virus, has become a potential target for design and synthesis of small molecule inhibit
Phenylpiperazine derivatives with a combination of partial dopamine-D2 receptor agonism and serotonin reuptake inhibition
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Page/Page column 27, (2010/11/08)
The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine-D2 receptors. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (1): wherein the symbols have the meanings given in the specification. and tautomers, stereoisomers and N-oxides thereof, as well as pharmacologically acceptable salts, hydrates and solvates of said compounds of formula (1) and its tautomers, stereoisomers and N-oxides.
2,4-DIAMINOQUINAZOLINES FOR SPINAL MUSCULAR ATROPHY
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Page/Page column 60, (2010/02/15)
2,4-Diaminoquinazolines of formulae I-IV and VI (I, II, III, IV and VI) are useful for treating spinal muscular atrophy (SMA).
