89122-67-8Relevant academic research and scientific papers
Preparation method of benzofuran derivative
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Paragraph 0054-0058, (2020/11/12)
The invention belongs to the field of organic chemical synthesis, and particularly relates to a preparation method of a benzofuran derivative. According to the specific technical scheme, the preparation method of the benzofuran derivative comprises the fo
Aryiolefins compound synthetic method
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Paragraph 0037; 0038; 0039; 0040, (2016/10/09)
The invention discloses an aryiolefins compound synthetic method and belongs to the field of organic chemistry synthesis. The aryiolefins compound synthetic method particularly includes dissolving an o-hydroxy (amino) aryl alkynes compound, a bis(pinacolato) borate compound, a transition metal (rhodium, iridium, palladium or platinum), alkali and a hydrogen source into an organic solvent at a nitrogen atmosphere prior to heating and stirring reaction, removing the organic solvent under reduced pressure after the reaction is terminated, and conducting column chromatography separation so as to obtain various o-hydroxy (amino) aryiolefins compounds. Compared with an existing method, the aryiolefins compound synthetic method has the advantages of simpler synthetic and reaction steps, mild reaction conditions, simplicity, convenience and feasibility in operation, cheap and easily available raw materials and capabilities of reaching more than 80% in product yield, inhibiting production of cyclization product benzofuran or indole derivatives and improving reaction efficiency and reactive atom economy, thereby being a novel approach to synthesis of the o-hydroxy (amino) aryiolefins compounds.
One-Step Synthesis of Substituted Benzofurans from ortho- Alkenylphenols via Palladium-Catalyzed C=H Functionalization
Yang, Dejun,Zhu, Yifei,Yang, Na,Jiang, Qiangqiang,Liu, Renhua
, p. 1731 - 1735 (2016/06/09)
A dehydrogenative oxygenation of C(sp2)=H bonds with intramolecular phenolic hydroxy groups has been developed, which provides a straightforward and concise access to structurally diversely benzofurans from ortho-alkenylphenols. The reaction is catalyzed by palladium on carbon (Pd/C) without any oxidants and sacrificing hydrogen acceptors.
Rhodium(III)-catalyzed C-H olefination for the Synthesis of ortho-alkenyl phenols using an oxidizing directing group
Shen, Yangyang,Liu, Guixia,Zhou, Zhi,Lu, Xiyan
, p. 3366 - 3369 (2013/07/26)
By using an oxidizing directing group, a mild, efficient Rh(III) catalyzed C-H olefination reaction between N-phenoxyacetamides and alkenes was developed. This reaction provided a straightforward way for the synthesis of ortho-alkenyl phenols, and the directing group is traceless in the product.
Synthesis, antitumor evaluation, and apoptosis-inducing activity of hydroxylated (E)-stilbenes
Lion, Cedric J.,Matthews, Charles S.,Stevens, Malcolm F. G.,Westwell, Andrew D.
, p. 1292 - 1295 (2007/10/03)
The parallel solution-phase synthesis of a series of 30 monohydroxylated (E)-stilbene analogues is described. In vitro screening revealed low micromolar activity (GI50) against the MDA MB 468 breast cancer cell line. Activity in MDA MB 468 cells correlated with the ability to induce apoptosis following drug treatment by the most potent agents in the series, e.g., 5dy and 5jy, an observation further reinforced by Annexin V-FITC analysis and fluorescence microscopy.
Syntheses and Platelet Aggregation Inhibitory and Antithrombotic Properties of ethyl>benzenes
Kikumoto, Ryoji,Hara, Hiroto,Ninomiya, Kunihiro,Osakabe, Masanori,Sugano, Mamoru,et al.
, p. 1818 - 1823 (2007/10/02)
A series of ethyl>benzene derivatives were synthesized and evaluated for their ability to inhibit collagen-induced platelet aggregation in vitro and to protect experimantal thrombosis in mice.The results showed that the compounds were in vitro inhibitors of collagen-induced platelet aggregation.Most of them were also effective in the mouse antithrombotic assay.The compounds were found to be potent antagonists to S2 serotonergic receptor, and good correlation (r = 0.85) between their S2 serotonergic receptor antagonism and their potency as platelet antiaggregatory drugs was observed.Among the compounds studied, monophenoxy>methyl>ethyl>succinate hydrochloride (12b, MCI-9042) was selected for further pharmacological and toxicological evaluation.
Preparation of (E)-2-Hxdroxy-4'-Substituted Stilbenes
Mylona, Anastasia,Nikokavouras, John,Takakis, Ioannis M.
, p. 3514 - 3530 (2007/10/02)
Sixteen (E)-2-hydroxy-4'-substituted stilbenes have been prepared by the Wittig reaction.Direct coupling of the appropriate p-substituted benzylidenetriphenylphosphoranes with salicylaldehyde afforded the (E)-stilbenols (2) 4'-R = H(2a), Me(2b), But(2c), Ph(2d), CN(2e), NO2(2i), OMe(2k), F(2n), Cl(2o), and Br(2p).Alternatively, the Wittig reaction of o-methoxymethoxybenzylidenetriphenylphosphorane with various p-substituted benzaldehydes gave the (E)-methoxymethylstilbenols (4) which upon acidic cleavage furnished the corresponding stilbenols (2) 4'-R = CN(2e), CO2Me(2f), NMe2(2h), OH(2j), OAc(2m), and I(2q).The symmetrical (E)-2,2'-dihydroxystilbene was obtained in an analogous fashion.Reduction of nitrostilbenol (2i) yielded the corresponding aminostilbenol (2g).
Substituted (ω-aminoalkoxy)stilbene derivatives as a new class of anticonvulsants
Kikumoto,Tobe,Fukami,Ninomiya,Egawa
, p. 645 - 649 (2007/10/02)
A series of substituted (ω-aminoalkoxy)stilbene derivatives has been synthesized and screened for anticonvulsant activity. The effect of structural modification of these molecules on the activities has been systematically examined. Potent anticonvulsant activity was displayed by 2-[4-(4-methyl-1-piperazinyl)butoxy]stilbene and some 2-[4-(3-alkoxy-1-piperidino)butoxy]stilbene derivatives, as determined by maximal electroshock seizure (MES) and pentylenetetrazol-induced convulsion tests in mice. One of these derivatives exhibited more potent anti-MES activity than diphenylhydantoin and carbamazepine in further pharmacological tests in rats, and its therapeutic index was superior to those of two antiepileptic drugs.
