128255-31-2Relevant academic research and scientific papers
Design and synthesis of chiral urea-derived iodoarenes and their assessment in the enantioselective dearomatizing cyclization of a naphthyl amide
Tariq, M.Umair,Moran, Wesley J.
, (2020)
A novel family of urea-derived chiral iodoarenes was designed and synthesized for use in enantioselective iodine(I/III) catalysis. Their preparation required the development of a bidirectional synthetic strategy. These new chiral iodoarenes were assessed as catalysts in the dearomatizing cyclization of a naphthyl amide and provided moderate yields of product in some cases with low enantioselectivities.
Metal-Free Tandem Approach for Triazole-Fused Diazepinone Scaffolds via [3 + 2]Cycloaddition/C-N Coupling Reaction
Majeed, Kashif,Wang, Lingna,Liu, Bangjie,Guo, Zijian,Zhou, Fengtao,Zhang, Qiuyu
, p. 207 - 222 (2020/12/23)
A novel metal-free, efficient cascade reaction has been developed to construct 1,2,3-triazole-fused 1,4-diazepinone skeletons. Mechanism investigation indicated that sodium azide has not only served as a 1,3-dipoles synthon in [3 + 2] cycloaddition but al
Synthesis and structure-activity relationship study of pyrrolidine-oxadiazoles as anthelmintics against Haemonchus contortus
Ruan, Banfeng,Zhang, Yuezhou,Tadesse, Solomon,Preston, Sarah,Taki, Aya C.,Jabbar, Abdul,Hofmann, Andreas,Jiao, Yaqing,Garcia-Bustos, Jose,Harjani, Jitendra,Le, Thuy Giang,Varghese, Swapna,Teguh, Silvia,Xie, Yiyue,Odiba, Jephthah,Hu, Min,Gasser, Robin B.,Baell, Jonathan
supporting information, (2020/02/04)
Parasitic roundworms (nematodes) are significant pathogens of humans and animals and cause substantive socioeconomic losses due to the diseases that they cause. The control of nematodes in livestock animals relies heavily on the use of anthelmintic drugs. However, their extensive use has led to a widespread problem of drug resistance in these worms. Thus, the discovery and development of novel chemical entities for the treatment of parasitic worms of humans and animals is needed. Herein, we describe our medicinal chemistry optimization efforts of a phenotypic hit against Haemonchus contortus based on a pyrrolidine-oxadiazole scaffold. This led to the identification of compounds with potent inhibitory activities (IC50 = 0.78–22.4 μM) on the motility and development of parasitic stages of H. contortus, and which were found to be highly selective in a mammalian cell counter-screen. These compounds could be used as suitable chemical tools for drug target identification or as lead compounds for further optimization.
Copper-Catalyzed Trifunctionalization of Alkynes: Rapid Formation of Oxindoles Bearing Geminal Diboronates
He, Tao,Li, Bin,Liu, Li-Chuan,Wang, Jing,Ma, Wen-Peng,Li, Guang-Yu,Zhang, Qing-Wei,He, Wei
supporting information, p. 966 - 970 (2019/01/04)
A copper-catalyzed trifunctionalization of alkynes that provides rapid access to oxindoles bearing a geminal diboronate side chain, highlighted by the simultaneous formation of one C?C bond and two C?B bonds, is reported. This new reaction features simple
NOVEL ALKENE OXINDOLE DERIVATIVES
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Page/Page column 35, (2011/04/18)
The present invention provides compounds of formula (I), as well as pharmaceutical acceptable salt thereof, wherein R1 to R7 have the significance given herein. The compounds are useful in the treatment of prophylaxis of diseases tha
NOVEL ALKENE OXINDOLE DERIVATIVES
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Page/Page column 71, (2011/04/19)
A compound of formula (I), the pharmaceutically acceptable salt, the pharmaceutical composition, the preparation method and the use thereof.
ALKENE OXINDOLE DERIVATIVES AND THEIR USES TO TREAT OBESITY, DIABETES AND HYPERLIPIDEMIA
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Page/Page column 69, (2011/04/19)
A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R7 have the significance given in claim 1, can be used as a medicament.
One-step synthesis of quinazolino[3,2-a ]quinazolinones via palladium-catalyzed domino addition/carboxamidation reactions
Zeng, Fanlong,Alper, Howard
supporting information; experimental part, p. 3642 - 3644 (2010/10/02)
A highly efficient palladium-catalyzed domino process has been developed for the synthesis of quinazolino[3,2-a]quinazolinones by forming five new bonds in a single step. Despite the high density and variety of functional groups on the substrates, the tetracyclic quinazolinones were obtained in good to excellent yields.
Stereoselective synthesis of 3-alkylideneoxindoles using tandem indium-mediated carbometallation and palladium-catalyzed cross-coupling reactions
Yanada, Reiko,Obika, Shingo,Kobayashi, Yusuke,Inokuma, Tsubasa,Oyama, Munetaka,Yanada, Kazuo,Takemoto, Yoshiji
, p. 1632 - 1642 (2007/10/03)
The first efficient methods for the stereoselective synthesis of various (E)-, (Z)-, and disubstituted 3-alkylideneoxindoles via radical cyclization reactions were investigated using tandem indium-mediated carbometallation and palladium-catalyzed cross-co
Studies on tellurium-containing heterocycles. Part 22. Tellurazepine ring system: Preparation of 1,5-benzotellurazepin-4-ones and their conversion into fully unsaturated 1,5-benzotellurazepines
Sashida, Haruki,Satoh, Hirohito
, p. 413 - 417 (2007/10/03)
The treatment of o-iodopropiolanilides (12), which were easily prepared from o-iodophenylisocyanate (11) and ethynylmagnesium bromide, with sodium hydrogen telluride resulted in the intramolecular ring closure of the presumed phenyltellurol intermediates (13) to a triple bond to give the 1,5-benzotellurazepin-4-ones (14) as the sole characterized products. The obtained amides (14) were easily converted into fully unsaturated lactim 4-methoxy-1,5-benzotellurazepines (18) by treatment with trimethyloxonium tetrafluoroborate. Decomposition by thermolysis of the 4-methoxyazepinenes (18) afforded the 4-methoxyquinolines (19) with extrusion of a tellurium atom.
