7114-80-9Relevant academic research and scientific papers
Rhodium(III)-Catalyzed C-H Activation: Annulation of Petrochemical Feedstocks for the Construction of Isoquinolone Scaffolds
Barber, Joyann S.,Kong, Dehuan,Li, Wei,McAlpine, Indrawan J.,Nair, Sajiv K.,Sakata, Sylvie K.,Sun, Nicole,Patman, Ryan L.
supporting information, p. 202 - 206 (2021/01/14)
We describe a simple and robust procedure for the Rh(III)-catalyzed [4+2] cycloaddition of feedstock gases enabled through C-H activation. A diverse set of 3,4-dihydroisoquinolones and 3-methylisoquinolones have been prepared in good to excellent yields.
Synthesis of rhodium(III)-catalyzed isoquinoline derivatives from allyl carbonates and benzimidates with hydrogen evolution
Dong, Lin,Li, Chao,Liu, Man,Xu, Hui-Bei,Zhang, Jing
, p. 1412 - 1416 (2020/03/03)
A novel Rh(iii)-catalyzed cascade C-H activation/cyclization approach to access isoquinoline derivatives from benzimidates and available allyl carbonates with the liberation of H2 has been realized. Allyl carbonates were first used as a versati
Iron-catalysed 1,2-acyl migration of tertiary α-azido ketones and 2-azido-1,3-dicarbonyl compounds
Yang, Tonghao,Lin, Yajun,Yang, Chaoqun,Yu, Wei
supporting information, p. 6097 - 6102 (2019/11/20)
Iron-catalysed 1,2-acyl migration of tertiary α-azido ketones and 2-azido-1,3-dicarbonyl compounds provides a simple and atom-economical approach toward enamides and isoquinolones. This paper reports two catalyst systems for these transformations which employ iron(ii) complexes [Fe(dpbz)]Br2 (dpbz = 1,2-bis(diphenylphosphino)benzene) and FeBr2/Et3N, respectively. [Fe(dpbz)]Br2 was found to be highly effective at converting 2-azido-2,3-dihydro-1H-inden-1-ones to isoquinolones. The reagent combination of FeBr2/Et3N, on the other hand, exhibited a broader catalytic scope, owing to the beneficial effect of Et3N. This latter catalyst system enables 2-azido-2-methyl-1,3-dicarbonyl compounds to be converted to the corresponding enamides under mild conditions in good yields.
Iron-Catalyzed Acyl Migration of Tertiary α-Azidyl Ketones: Synthetic Approach toward Enamides and Isoquinolones
Yang, Tonghao,Fan, Xing,Zhao, Xiaopeng,Yu, Wei
, p. 1875 - 1879 (2018/04/16)
This paper reports that tertiary α-azidyl phenyl ketones can be transformed into enamides by treatment with FeBr2 at elevated temperature in DMF. The reaction proceeds via 1,2-benzoyl migration from α-carbon to the nitrogen atom, accompanied by expulsion of a nitrogen molecule. This protocol is suitable for the synthesis of N-(cyclopent-1-en-1-yl)benzamides, N-(cyclohex-1-en-1-yl)benzamides, and N-benzoyl-α-methyl enamines and provides a convenient approach toward isoquinolones.
USE OF DDX3 INHIBITORS AS ANTIPROLIFERATIVE AGENTS
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Page/Page column 83; 84, (2017/10/30)
The present invention refers to compounds of formula I or II endowed with DDX3 inhibitory activity, relative pharmaceutical compositions and their use as antihyperproliferative agents. (I) or (II)
HUMAN HELICASE DDX3 INHIBITORS AS THERAPEUTIC AGENTS
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Page/Page column 91, (2016/09/22)
The present invention refers to compounds endowed with RNA helicase DDX3 inhibitory activity of formula I and II and their therapeutic use, in particular for the treatment of viral diseases.
Synthesis of functionalized isoquinolin-1(2H)-ones by copper-catalyzed α-arylation of ketones with 2-halobenzamides
Shi, Yan,Zhu, Xuebin,Mao, Haibin,Hu, Hongwen,Zhu, Chengjian,Cheng, Yixiang
supporting information, p. 11553 - 11557 (2013/09/12)
Copper is key: A concise route to isoquinolin-1(2H)-ones from simple and readily available starting materials is provided by an efficient copper-catalyzed annulation of ketones with 2-halobenzamides. The method is applicable to a wide range of ketones con
The design, synthesis and structure-activity relationships of 1-aryl-4-aminoalkylisoquinolines: A novel series of CRF-1 receptor antagonists
Yoon, Taeyoung,De Lombaert, Stephane,Brodbeck, Robbin,Gulianello, Michael,Chandrasekhar, Jayaraman,Horvath, Raymond F.,Ge, Ping,Kershaw, Mark T.,Krause, James E.,Kehne, John,Hoffman, Diane,Doller, Dario,Hodgetts, Kevin J.
, p. 891 - 896 (2008/09/18)
The design, synthesis and structure-activity relationships of a novel series of CRF-1 receptor antagonist, the 1-aryl-4-alkylaminoisoquinolines, is described. The effects of substitution on the aromatic ring, the amino group and the isoquinoline core on C
1-ARYL-4-SUBSTITUTED ISOQUINOLINES
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, (2010/02/14)
1-Aryl-4-substituted isoquinolines analogues of Formula (I) and Formula (II) are provided, as follows : wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula (I) and (II) bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 1-aryl-4-substituted isoquinolines, which are useful as probes for the localization of C5a receptors.
Poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors based on a tetrahydro-1(2H)-isoquinolinone Scaffold: Synthesis, biological evaluation and X-ray crystal structure
Peukert, Stefan,Schwahn, Uwe,Guessregen, Stefan,Schreuder, Herman,Hofmeister, Armin
, p. 1550 - 1554 (2007/10/03)
The synthesis, activity and physical properties of two series of novel potent tetrahydro-1(2H)-isoquinolinone based PARP-1 inhibitors are described. The new structural classes with a non-planar ring system interact specifically with the PARP-1 protein at the nicotinamide-binding site. Georg Thieme Verlag Stuttgart.
