6698-72-2Relevant academic research and scientific papers
TBAI/TBHP mediated oxidative cross coupling of ketones with phenols and carboxylic acids: Direct access to benzofurans
Santhosh Kumar,Ravikumar,Chinna Ashalu,Rajender Reddy
supporting information, p. 33 - 37 (2017/12/11)
TBAI/TBHP mediated oxidative cross coupling of phenols and carboxylic acids with ketones has been reported under metal-free, base free, solvent free conditions enabling environmentally benign synthesis of aryloxyketones, acyloxy ketones and benzofurans. Phenoxyketones and acyloxylcarbonyl compounds were synthesized in good to high yields, where as benzofurans were synthesized in moderate yields. This method is operationally simple, works under mild conditions, using commercially available as well as inexpensive TBAI and an oxidant TBHP.
Design and synthesis of new RAF kinase-inhibiting antiproliferative quinoline derivatives. Part 2: Diarylurea derivatives
El-Gamal, Mohammed I.,Khan, Mohammad Ashrafuddin,Tarazi, Hamadeh,Abdel-Maksoud, Mohammed S.,Gamal El-Din, Mahmoud M.,Yoo, Kyung Ho,Oh, Chang-Hyun
, p. 413 - 423 (2017/01/13)
This article describes the design, synthesis, and biological screening of a new series of diarylurea derivatives possessing quinoline nucleus. Nine target compounds were selected by the National Cancer Institute (NCI, Bethesda, Maryland, USA) for in?vitro antiproliferative screening against a panel of 58 cancer cell lines of nine cancer types. Following one-dose initial screening, compounds 1d-g and 2b were selected for 5-dose screening in order to calculate their IC50and total growth inhibition (TGI) values against the cell lines. Compounds 1e and 1g were the most promising analogues. Both compounds showed strong potency and broad-spectrum antiproliferative activity against the different tested cancer types. Their IC50and TGI values were less than those of the reference drug, sorafenib, against most of the tested cell lines of the nine different cancer types. Furthermore, the most potent compounds 1d-g were tested against C-RAF kinase as a potential molecular target of this series of compounds. All of them showed high potency, and the most potent derivative was compound 1e (IC50?=?0.10?μM). It was further tested against a panel of another twelve kinases, and it showed selectivity against C-RAF kinase. This could be, at least in part, the possible mechanism of antiproliferative action of this series of compounds at molecular level. The binding modes of compounds 1e and 1g were studied by docking studies, which highlighted the importance of the urea linker compared with the amide linker.
METHOD FOR PRODUCING PYRIMIDINE-1-OL COMPOUND, AND INTERMEDIATE THEREOF
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Paragraph 0053-0055, (2017/08/07)
There are provided a method for producing 2,4-disubstituted pyrimidine-5-ol, and particularly, 2,4-dimethylpyrimidine-5-ol and an intermediate thereof used in industrial production. The production method according to the present invention includes a step
Silver-containing microemulsion as a high-efficient and recyclable catalytic system for hydration of alkynes
Dong, Qizhi,Li, Ningbo,Qiu, Renhua,Wang, Jinying,Guo, Cancheng,Xu, Xinhua
, p. 122 - 127 (2015/10/12)
A silver-catalyzed highly efficient and regioselective synthesis of ketones from a wide range of alkynes is described. The reaction is dramatically accelerated by its performance in aqueous emulsion, which is self-assembled by the addition of silver perfluorooctanesulfonate (1) and perfluorooctanesulfonic acid (PFOS) to water. The reaction is conducted under convenient conditions with broad substrate scope, including a variety of aromatic and aliphatic terminal alkynes and internal alkynes. Furthermore, the air- and light-stable silver catalytic microemulsion can be reused for 4 times with minimal change in catalytic efficiency.
Linear Free Energy Correlation Analysis on the Electronic Effects of Rh(II) Carbene O-H Insertion
Qu, Zhaohui,Shi, Weifeng,Wang, Jianbo
, p. 217 - 219 (2007/10/03)
The relative rate constants for the Rh(II)-catalyzed insertion of diazoacetone into the O-H bond have been measured through intermolecular competitions. The kinetic data were subjected to Hammett correlation analysis, and mechanistic implication of the results with respect to a stepwise vs a concerted O-H insertion pathway is discussed.
Oxidative process for the preparation of allyl quinone derivatives
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, (2008/06/13)
A process for the industrial preparation of the quinone derivative represented by the following general formula: STR1 which is an intermediate for chroman derivatives useful as a blood sugar lowering agent, and novel intermediates, encompasses the followi
POLYMER-SUPPORTED REAGENTS: AN EFFICIENT METHOD FOR THE SYNTHESIS OF PHENOXYACETONES
Salunkhe, Deepak,Jagdale, Mansingrao,Mane, Ramchandra,Salunkhe, Manikrao
, p. 411 - 412 (2007/10/02)
Phenoxides supported on Amberlite IRA-400 reacted with chloroacetone to give the corresponding phenoxyacetones in high yields and purity.
Isocarbostyril derivatives
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, (2008/06/13)
Compounds of the structure STR1 wherein X, R1, R2, R3, R4, and R5 are as herein defined, effective as β-blockers and hypotensive agents, are described.
