89999-70-2Relevant academic research and scientific papers
Reductive Coupling between C-N and C-O Electrophiles
He, Rong-De,Li, Chun-Ling,Pan, Qiu-Quan,Guo, Peng,Liu, Xue-Yuan,Shu, Xing-Zhong
supporting information, p. 12481 - 12486 (2019/09/04)
The cross-electrophile reaction is a promising strategy for C-C bond formation. Recent studies have focused mainly on reactions with organic halides. Here we report a coupling reaction between C-N and C-O electrophiles that demonstrates the possibility of constructing a C-C bond via C-N and C-O cleavage. Several reactions between benzyl/aryl ammonium salts and vinyl/aryl C-O electrophiles have been studied. Preliminary mechanistic studies revealed that the benzyl ammoniums were activated through a radical mechanism.
OXABOROLE ESTERS AND USES THEREOF
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Page/Page column 68; 69, (2017/12/05)
The present invention provides oxaborole ester compounds and compositions thereof which are useful to treat diseases associated with parasites, such as Chagas Disease and African Animal Trypanosomosis.
Simple Amine-Directed Meta-Selective C-H Arylation via Pd/Norbornene Catalysis
Dong, Zhe,Wang, Jianchun,Dong, Guangbin
supporting information, p. 5887 - 5890 (2015/05/27)
Herein we report a highly meta-selective C-H arylation using simple tertiary amines as the directing group. This method takes advantage of Pd/norbornene catalysis, offering a distinct strategy to control the site selectivity. The reaction was promoted by commercially available AsPh3 as the ligand and a unique "acetate cocktail". Aryl iodides with an ortho electron-withdrawing group were employed as the coupling partner. A wide range of functional groups, including some heteroarenes, are tolerated under the reaction conditions. In addition, the amine directing group can be easily installed and transformed to other common versatile functional groups. We expect this C-H functionalization mode to have broad implications for developing other meta-selective transformations beyond this work.
Design, synthesis and evaluation of novel HDAC inhibitors as potential antitumor agents
Cheng, Jianjun,Qin, Jihong,Guo, Sihua,Qiu, Hangdeng,Zhong, Yun
, p. 4768 - 4772 (2015/01/09)
Phenyl imidazolidin-2-one was introduced as the linker for novel HDAC inhibitors. A focused library of 20 compounds was designed and synthesized, among which eight compounds showed equivalent or higher potencies against HDAC1 as compared to vorinostat. In vitro antitumor activity assays in HCT-116, PC-3 and HL-60 cancer cells revealed six compounds with potent antitumor activities, and compound 1o showed 6- to 9-fold higher potencies compared to vorinostat. In an HCT-116 nude mice xenograft model, compound 1o displayed significant antitumor activity in both continuous and intermittent dosing schedules.
NOVEL COMPOUNDS
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Page/Page column 70-71, (2012/03/26)
Disclosed are retinoid-related orphan receptor gamma (RORγ) modulators and their use in the treatment of diseases mediated by RORγ.
Discovery of novel thieno[2,3-d]pyrimidin-4-yl hydrazone-based inhibitors of Cyclin D1-CDK4: Synthesis, biological evaluation and structure-activity relationships. Part 2
Horiuchi, Takao,Nagata, Motoko,Kitagawa, Mayumi,Akahane, Kouichi,Uoto, Kouichi
experimental part, p. 7850 - 7860 (2010/04/02)
The design, synthesis and evaluation of novel thieno[2,3-d]pyrimidin-4-yl hydrazone analogues as cyclin-dependent kinase 4 (CDK4) inhibitor are described. Focusing on the optimization of the heteroaryl moiety at the hydrazone with substituted phenyl group
Design, synthesis and AChE inhibitory activity of indanone and aurone derivatives
Sheng, Rong,Xu, Yu,Hu, Chunqi,Zhang, Jing,Lin, Xiao,Li, Jingya,Yang, Bo,He, Qiaojun,Hu, Yongzhou
experimental part, p. 7 - 17 (2009/04/06)
A new series of indanone and aurone derivatives have been synthesized and tested for in vitro AChE inhibitory activity by modified Ellman method. Most of them exhibit AChE inhibitory activities superior to rivastigmine. Further, the most potent compound 1g was selected to evaluate the effect on the acquisition and memory impairment by mice step-down passive avoidance test.
Triazole derivatives
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, (2011/03/17)
The present invention relates to triazole and imidazole derivatives of formula I and to their pharmaceutically acceptable acid addition salts. These compounds are NMDA receptor subtype blockers and are useful for the treatment of diseases related to the NMDA receptor.
Benzodiazepine derivatives useful as CCK-receptor antagonists
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, (2008/06/13)
This invention relates to benzodiazepine derivatives which are useful as drugs exhibiting antagonism at the gastrin and/or CCK-B receptor, and to their production.
Structure-activity, theoretical, and X-ray studies on the intramolecular interactions in a series of novel histamine H2 receptor antagonists
Lumma Jr.,Baldwin,Bicking,Bolhofer,Hoffman,Phillips,Robb,Torchiana,Schlegel,Smith
, p. 1047 - 1052 (2007/10/02)
The furan ring of the histamine H2 receptor antagonist 3-amino-4-[[2-[[[5-[(dimethylamino)methyl]-2-furanyl]-methyl]thio]ethyl]am ino]-1,2,5-thiadiazole 1-oxide (1a) was replaced by thiophene, pyridine, benzene, and pyrrole. The relative recept
