2303-23-3Relevant academic research and scientific papers
Diaryl ether compound, preparation method and application thereof
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Paragraph 0107-0109; 0116, (2019/01/23)
The invention relates to a diaryl ether compound , a preparation method and application thereof, wherein the diaryl ether compound has the following structural formula: (the formula is shown in the description), wherein, -X- is CH- or -N-; =R1,-R2,-R3 are independently selected from one kind of H-,-F,-Cl,-Br, alkoxy, aryl, aryloxy, N, N-Dialkylamino, N-Alkyl-N-Acylamino, pyridyl, imidazolyl, pyrazolyl, furyl, pyrrolyl, morpholinyl, N-Alkyl piperazinyl, piperidinyl and tetrahydropyrrolyl. The diaryl ether compound has the advantage of inhibiting the activity of a PFKFB3 in the tumor cells, effectively blocking the activation of the key enzyme during the glycolysis process, thereby blocking energy supply from the energy source of the tumor cells, and providing a new medicament for the effective treatment of the tumor diseases.
CsF/clinoptilolite: An efficient solid base in SNAr and copper-catalyzed Ullmann reactions
Keipour, Hoda,Hosseini, Abolfazl,Afsari, Amir,Oladee, Razieh,Khalilzadeh, Mohammad A.,Ollevier, Thierry
, p. 95 - 104 (2016/01/16)
CsF/clinoptilolite was found to be an efficient solid base catalyst for both SNAr and Ullmann ether reactions. A general and efficient one-step procedure was developed for the synthesis of biaryl ethers via direct coupling of electron-deficient aryl halides to phenols using CsF/clinoptilolite. The protocol was also applied to electron-rich aryl halides by addition of a catalytic amount of copper oxide nanoparticles. Both SNAr and Ullmann reactions were rapid and provided good to excellent yields.
Synthesis and biological evaluation of pentanedioic acid derivatives as farnesyltransferase inhibitors
Yang, Liuqing,Liu, Wei,Mei, Hanbing,Zhang, Yuan,Yu, Xiaojuan,Xu, Yufang,Li, Honglin,Huang, Jin,Zhao, Zhenjiang
supporting information, p. 671 - 676 (2015/04/27)
Structure-based virtual screening of a commercial library identified pentanedioic acid derivatives (6 and 13b) as a kind of novel scaffold farnesyltransferase inhibitors (FTIs). Chemical modifications of the lead compounds, biological assays and analysis of the structure-activity relationships (SAR) were conducted to discover more potent FTIs. Some of them displayed excellent inhibition against FTase, and among them, the most active compound 13n with an IC50 value of 0.0029 μM and SAR analysis might be helpful to the discovery of more potent FTIs. This journal is
P(i-BuNCH2CH2)3N: an efficient promoter for the microwave synthesis of diaryl ethers
Raders, Steven M.,Verkade, John G.
, p. 3507 - 3511 (2008/09/21)
With the title proazaphosphatrane as a promoter, the coupling of aryl fluorides with aryl TBDMS ethers under microwave conditions gave moderate to high yields of the desired products at low catalyst loadings and in short times. In this methodology, electron deficient aryl fluorides possessing substituents, such as nitro, cyano, and ester, were coupled with sterically demanding aryl TBDMS ethers as well as with aryl TBDMS ethers bearing a variety of functionalities such as methoxy, halo, and cyano groups.
P(i-BuNCH2CH2)3N: An efficient promoter for the nucleophilic aromatic substitution reaction of aryl fluorides with aryl TBDMS (or TMS) ethers
Urgaonkar, Sameer,Verkade, John G.
, p. 3319 - 3322 (2007/10/03)
(Chemical Equation Presented) The nucleophilic aromatic substitution reaction between electron-deficient aryl fluorides and aryl TBDMS (or TMS) ethers has been shown to be efficiently promoted by proazaphosphatranes such as P(i-BuNCH2CH2)3N (3). Excellent yields of diaryl ether products were obtained under unusually mild conditions.
