- Structural Insights into the TES/TFA Reduction of Differently Substituted Benzofurans: Dihydrobenzofurans or Bibenzyls?
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Various polysubstituted benzofurans were reduced by using triethylsilane in trifluoracetic acid. 2,3-Dihydrobenzofurans or bibenzyl compounds were obtained in high yields, depending on the nature of the substituents at C2 and on the benzene ring of the co
- D'Orsi, Rosarita,Caivano, Ilaria,Funicello, Maria,Lupattelli, Paolo,Chiummiento, Lucia
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supporting information
p. 63 - 64
(2020/11/04)
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- Synthesis and biological evaluation of 2-arylbenzofuran derivatives as potential anti-Alzheimer’s disease agents
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Alzheimer's disease (AD) is a type of progressive dementia caused by degeneration of the nervous system. A single target drug usually does not work well. Therefore, multi-target drugs are designed and developed so that one drug can specifically bind to mu
- Yun, Yinling,Miao, Yuhang,Sun, Xiaoya,Sun, Jie,Wang, Xiaojing
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p. 1346 - 1356
(2021/06/26)
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- Synthesis of Benzofurans from Ketones and 1,4-Benzoquinones
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Benzofuran derivatives can be synthesized through the sequential Michael addition and cyclization of 1,3-dicarbonyl compounds with 1,4-benzoquinones. However, ketones are rarely used in this reaction because of their low nucleophilicities. In this study, this problem was solved by utilizing triethyl orthoformate, which enabled the formation of a vinyl ethyl ether as an additive. As a result, the nucleophilicity of ketones increased. Many important 5-hydroxybenzofuran derivatives, which were not readily available by synthesis in the past, were also prepared via these newly established reactions. (Figure presented.) .
- Wu, Fengtian,Bai, Rongxian,Gu, Yanlong
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p. 2307 - 2316
(2016/07/29)
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- General method for functionalized polyaryl synthesis via aryne intermediates
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A method for base-promoted arylation of arenes and heterocycles by aryl halides and aryl triflates is described. Additionally, in situ electrophilic trapping of ArLi intermediates generated in the reaction of benzyne with deprotonated arenes or heterocycles has been developed, providing rapid and easy access to a wide range of highly functionalized polyaryls. Base-promoted arylation methodology complements transition-metal-catalyzed direct arylation and allows access to structures that are not easily accessible via other direct arylation methods. The reactions are highly functional-group tolerant, with alkene, ether, dimethylamino, trifluoromethyl, ester, cyano, halide, hydroxyl, and silyl functionalities compatible with reaction conditions.
- Truong, Thanh,Mesgar, Milad,Le, Ky Khac Anh,Daugulis, Olafs
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supporting information
p. 8568 - 8576
(2014/07/07)
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- A direct approach to 5-hydroxybenzofurans via a platinum-catalyzed domino rearrangement/5-endo-dig cyclization reaction of quinols
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(Chemical Equation Presented) A highly efficient and atom-economical construction of 2-substituted 5-hydroxybenzofurans was accomplished by employing a platinum-catalyzed domino dienone-phenol rearrangement/5-endo-dig cyclization reaction of quinols beari
- Kim, Ikyon,Kim, Kyungsun,Choi, Jungeun
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supporting information; experimental part
p. 8492 - 8495
(2010/03/01)
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- A new synthetic access to furo[3,2-f]chromene analogues of an antimycobacterial
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From the structure of 3,3-dimethyl-3H-benzofuro[3,2-f][1]-benzopyran, a selective in vitro inhibitor of mycobacterial growth, we have undertaken a structure-activity relationship investigation. We wish to report here our results on the use of [2+3] cycloadditions between 2-formylbenzoquinone and various enol derivatives to give various 4-formyl-5-hydroxy benzofurans. In the next step, an ytterbium triflate-catalysed reaction with 2-methylpropene allowed the preparation of various original furo[3,2-f]chromenes derivatives. Their biological evaluation on the growth of Mycobacterium smegmatis as well as Mycobacterium tuberculosis pointed out that some analogues were four times more active than the initial hit.
- Alvey, Luke,Prado, Soizic,Huteau, Valerie,Saint-Joanis, Brigitte,Michel, Sylvie,Koch, Michel,Cole, Stewart T.,Tillequin, Francois,Janin, Yves L.
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experimental part
p. 8264 - 8272
(2009/04/11)
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- INDANE AND TETRAHYDRONAPHTHALENE DERIVATIVES AS CALCIUM CHANNEL ANTAGONISTS
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This invention describes the use of aminoindane and amino-tetrahydronaphthalene derivatives of general formula (I) STR1 in which Ar, X, R 1, R 2 and n are defined in claim 1, for the manufacture of a medicament for the treatment of disorders in which a calcium channel antagonist is indicated. Novel compounds falling within formula (I) are also claimed.
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