- Preparation method of benzofuran derivative
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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
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Paragraph 0054-0058
(2020/11/12)
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- Late-Stage Direct o-Alkenylation of Phenols by PdII-Catalyzed C?H Functionalization
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o-Alkenylation of unprotected phenols has been developed by direct C?H functionalization catalyzed by PdII. This work features phenol group as a directing group and realizes highly site-selective C?H bond functionalization of phenols to achieve the corresponding products in moderate to excellent yields at 60 °C. The advantages of this reaction include unprecedented C?H functionalization using phenol as a directing group, high regioselectivity, good substrate scope, mild reaction conditions, and high efficiency. To the best of our knowledge, this is the first example of a regioselective C?H alkenylation of unprotected phenols utilizing phenolic hydroxyl group as a directing group. The alkenylation of unprotected tyrosine and intramolecular cyclization are also successfully carried out under this catalytic system in good yields. Furthermore, this novel method enables a late-stage modification of complex phenol-containing bioactive molecules toward a diversity-oriented drug discovery.
- Dou, Yandong,Kenry,Liu, Jiang,Jiang, Jianze,Zhu, Qing
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supporting information
p. 6896 - 6901
(2019/05/07)
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- Hypervalent Iodine(III)-Catalyzed Synthesis of 2-Arylbenzofurans
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An alternative route for the synthesis of 2-arylbenzofurans is described by iodine(III)-catalyzed oxidative cyclization of 2-hydroxystilbenes using 10 mol% (diacetoxyiodo)benzene [PhI(OAc) 2 ] as catalyst in the presence of m -chloroperbenzoic acid. The 2-arylbenzofurans were isolated in good to excellent yields.
- Singh, Fateh V.,Mangaonkar, Saeesh R.
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p. 4940 - 4948
(2018/12/14)
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- Hypervalent iodine mediated oxidative cyclization of o -hydroxystilbenes into benzo- and naphthofurans
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A new and convenient metal-free cyclization of ortho-hydroxystilbenes into 2-arylbenzofurans and 2-arylnaphthofurans mediated by hypervalent iodine reagents is described. The cyclization products are isolated in good to excellent yields using stoichiometric (diacetoxyiodo)benzene in acetonitrile. Georg Thieme Verlag Stuttgart New York.
- Singh, Fateh V.,Wirth, Thomas
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experimental part
p. 1171 - 1177
(2012/05/20)
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- Preparation of (E)-2-Hxdroxy-4'-Substituted Stilbenes
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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).
- Mylona, Anastasia,Nikokavouras, John,Takakis, Ioannis M.
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p. 3514 - 3530
(2007/10/02)
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- Substituted (ω-aminoalkoxy)stilbene derivatives as a new class of anticonvulsants
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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.
- Kikumoto,Tobe,Fukami,Ninomiya,Egawa
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p. 645 - 649
(2007/10/02)
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