40915-37-5Relevant academic research and scientific papers
Computational and experimental studies on copper-mediated selective cascade C-H/N-H annulation of electron-deficient acrylamide with arynes
Chen, Chao,Hao, Yu,Zhang, Ting-Yu,Pan, Jin-Long,Ding, Jun,Xiang, Heng-Ye,Wang, Man,Ding, Tong-Mei,Duan, Abing,Zhang, Shu-Yu
supporting information, p. 755 - 758 (2019/01/21)
An efficient and convenient copper-mediated method has been developed to achieve direct cascade C-H/N-H annulation to synthesize 2-quinolinones from electron-deficient acrylamides and arynes. This method highlights an emerging but simple strategy to transform inert C-H bonds into versatile functional groups in organic synthesis to provide a new method of synthesizing 2-quinolinones efficiently. Mechanistic investigations by experimental and density functional theory (DFT) studies suggest that an organometallic C-H activation via a Cu(iii) intermediate is likely to be involved in the reaction.
Synthesis and neuroprotective action of xyloketal derivatives in Parkinson's disease models
Li, Shichang,Shen, Cunzhou,Guo, Wenyuan,Zhang, Xuefei,Liu, Shixin,Liang, Fengyin,Xu, Zhongliang,Pei, Zhong,Song, Huacan,Qiu, Liqin,Lin, Yongcheng,Pang, Jiyan
, p. 5159 - 5189 (2014/02/14)
Parkinson's disease (PD) is the second most common neurodegenerative disease affecting people over age 55. Oxidative stress actively participates in the dopaminergic (DA) neuron degeneration of PD. Xyloketals are a series of natural compounds from marine mangrove fungus strain No. 2508 that have been reported to protect against neurotoxicity through their antioxidant properties. However, their protection versus 1-methyl-4-phenylpyridinium (MPP+)-induced neurotoxicity is only modest, and appropriate structural modifications are necessary to discover better candidates for treating PD. In this work, we designed and synthesized 39 novel xyloketal derivatives (1-39) in addition to the previously reported compound, xyloketal B. The neuroprotective activities of all 40 compounds were evaluated in vivo via respiratory burst assays and longevity-extending assays. During the zebrafish respiratory burst assay, compounds 1, 9, 23, 24, 36 and 39 strongly attenuated reactive oxygen species (ROS) generation at 50 μM. In the Caenorhabditis elegans longevity-extending assay, compounds 1, 8, 15, 16 and 36 significantly extended the survival rates (p +). In the MPP+-induced C57BL/6 mouse PD model, 40 mg/kg of 1 and 8 protected against MPP+-induced dopaminergic neurodegeneration and increased the number of DA neurons from 53% for the MPP+ group to 78% and 74%, respectively (p 0.001 vs. MPP+ group). Thus, these derivatives are novel candidates for the treatment of PD.
IMIDAZOTRIAZINONE COMPOUNDS
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Paragraph 0561; 0562, (2013/10/08)
The present invention provides imidazotriazinone compounds which are inhibitors of phosphodiesterase 9 and pharmaceutically acceptable salt thereof. The present invention further provides processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of PDE9 associated diseases or disorders in mammals, including humans.
IMIDAZOTRIAZINONE COMPOUNDS
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Page/Page column 99-100, (2012/04/10)
The present invention provides imidazotriazinone compounds which are inhibitors of phosphodiesterase 9. The present invention further provides processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of PDE9 associated diseases or disorders in mammals, including CNS or neurodegeneration disorder.
The reaction of 3,4-dihydro-2H-pyran with oxalyl chloride: Formation and crystal structure analysis of an unexpected bicyclic product
Schmidt, Bernd,Werner, Frank,Kelling, Alexandra,Schildeb, Uwe
experimental part, p. 1171 - 1175 (2010/11/16)
(Chemical Equation Presented) 3,4-Dihydro-2-H-pyran and oxalyl chloride react, depending on the conditions, to keto esters, a pyran-3-carboxylic acid or derivatives thereof, or to an hitherto unknown bicyclic acetal containing a vinyl chloride moiety. The structure of the latter product has been unambiguously elucidated by single-crystal X-ray structure analysis. A mechanism for its formation is proposed.
The enantioselective hydrogenation of 5,6-dihydro-2H-pyran-3-carboxylic acid over a cinchona alkaloid-modified palladium catalyst: Asymmetric synthesis of a cockroach attractant
Szori, Kornel,Szollosi, Gyoergy,Bartok, Mihaly
scheme or table, p. 1354 - 1358 (2009/02/04)
A novel application of a cinchona-modified supported Pd catalyst is presented. The key step in the asymmetric synthesis of the cockroach attractant methyl (+)-tetrahydro-2H-pyran-3-carboxylate was the enantioselective hydrogenation of 5,6-dihydro-2H-pyran
A New Indirect Application of Aggregative Activation: Synthesis of Esters by Cobalt-Catalyzed Carbonylation of Aryl, Heterocyclic, and Vinyl Halides under Atmospheric Pressure
Marchal, Joel,Bodiguel, Jacques,Fort, Yves,Caubere, Paul
, p. 8336 - 8340 (2007/10/02)
Sun lamp illuminated alkoxycarbonylation of aryl, heteroaryl, and vinyl halides was performed under atmospheric pressure of CO in the presence of a cobalt catalyst in situ generated from Co(OAc)2.Illunination through a Pyrex flask was sufficient to catalyze the reaction.This process avoids the use of Co2(CO)8 and excess CH3I, which were required in the earlier procedure.A SRN1 mechanism is proposed.
A Convenient Synthetic Method for β-Alkoxy- and β-Phenoxyacrylic Acids and 3,4-Dihydro-2H-pyran-5- and 2,3-Dihydrofuran-4-carboxylic Acids
Hojo, Masaru,Masuda, Ryoichi,Sakaguchi, Syuhei,Takagawa, Makoto
, p. 1016 - 1017 (2007/10/02)
trans-β-Trihaloacetylvinyl ethers 1 are easily hydrolyzed by wet potassium hydroxide in benzene, yielding the corresponding acids 2 in excellent yields.This synthetic method also can be applicable to cyclic vinyl ethers 3 and 5 to yield 4 and 6 in high yi
