23911-56-0Relevant academic research and scientific papers
Bi(OTf)3-Mediated (4+1) Annulation of α-Sulfonyl o-Hydroxyacetophenones with α-Hydroxy Arylketones to Access Sulfonyl 2-Aroylbenzofurans
Chang, Meng-Yang,Chen, Kuan-Ting
, p. 2594 - 2609 (2021/03/29)
In this paper, a high-yield, facile route for the scalable synthesis of sulfonyl 2-aroylbenzofurans via a Bi(OTf)3-mediated intermolecular double cyclocondensation of α-sulfonyl o-hydroxyacetophenones with substituted α-hydroxy arylketones under mild open-vessel reaction conditions is described. In the overall reaction, water is generated as the only byproduct. Various metal triflate-promoted reactions and conditions are investigated for the efficient one-pot (4+1) annulation reaction. (Figure presented.).
TRANSCRIPTION FACTOR BRN2 INHIBITORY COMPOUNDS AS THERAPEUTICS AND METHODS FOR THEIR USE
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Page/Page column 79, (2020/05/15)
The invention provides a variety of compounds having the structure of Formula I and uses of such compounds for treatment of various indications, including cancer as well as methods of treatment involving such compounds are also provided. The uses of the compounds may specifically include: bladder cancer, cholangiocarcinoma; colorectal cancer; diffuse large B-cell lymphoma (DLBC); liver cancer; ovarian cancer; thymoma; thyroid cancer; clear cell renal cell carcinoma (CCRCC); chromophobe renal cell carcinoma (ChRCC); prostate cancer; breast cancer; uterine cancer; pancreatic cancer; cervical cancer; uveal melanoma; acute myeloid leukemia (AML); head and neck cancer; small cell lung cancer (SCLC); lung adenocarcinoma sarcoma; mesothelioma; adenoid cystic carcinoma (ACC), sarcoma; testicular germ cell cancer; uterine cancer; pheochromocytoma and paraganglioma (PCPG); melanoma; glioma; glioblastoma multiforme; T-cell Acute Lymphoblastic Leukemia; T-cell Lympohoma, medulloblastoma; and neuroblastoma.
Synthesis, biological evaluation and molecular dynamic simulations of novel Benzofuran-tetrazole derivatives as potential agents against Alzheimer's disease
Kushwaha, Pragati,Fatima, Soobiya,Upadhyay, Akanksha,Gupta, Sampa,Bhagwati, Sudha,Baghel, Tanvi,Siddiqi,Nazir, Aamir,Sashidhara, Koneni V.
supporting information, p. 66 - 72 (2018/11/23)
A series of novel Benzofuran-tetrazole derivatives were successfully synthesised by integrating multicomponent Ugi-azide reaction with the molecular hybridization approach. Interestingly, a number of synthesized derivatives (5c, 5d, 5i, 5l, 5q and 5s) exhibited significant reduction of aggregation of “human” amyloid beta peptide, expressing on transgenic Caenorhabditis elegans (C. elegans) strain CL4176. Further, in silico docking results have evidenced the exquisite interaction of active compounds with the help of TcAChE–E2020 complex. These findings underscore the potential of these hybrids as lead molecules against Alzheimers's disease.
Facile microwave-assisted synthesis of substituted benzofuran derivatives
Liu, Junqiang,Mi, Chenggen,Tang, Xuemei,Cao, Yuan,Li, Zicheng,Huang, Wencai
, p. 2083 - 2090 (2014/05/06)
A series of benzofuran derivatives have been synthesized by use of a microwave-assisted process. Substituted or unsubstituted ?- hydroxyacetophenone and salicylaldehyde reacted with ethyl bromoacetate, ω-bromoacetophenone, or chloroacetone under the action of potassium carbonate in DMF to yield substituted benzofuran derivatives. Compared with conventional heating, this microwave-assisted synthetic process has the advantages of more convenient operation, shorter reaction time, and higher yield.
Preparation of highly functionalised benzofurans from ortho-hydroxyphenones and dichloroethylene: Applications and mechanistic investigations
Schevenels, Florian,Tinant, Bernard,Declercq, Jean-Paul,Markó, István E.
, p. 4335 - 4343 (2013/04/24)
Highly functionalised benzofurans have been prepared from ortho-hydroxyphenones and 1,1-dichloroethylene. The key intermediate, a chloromethylene furan, smoothly rearranged into the corresponding benzofuran carbaldehyde under acidic conditions. Some mechanistic investigations have been performed and several biologically active benzofurans have been synthesised. Copyright
Efficient and connective assembly of highly functionalized benzofurans using o-hydroxyphenones and dichloroethylene
Schevenels, Florian,Marko, Istvan E.
, p. 1298 - 1301 (2012/05/31)
The preparation of highly functionalized benzofurans by a unique and connective transformation is reported. Base-catalyzed condensation of o-hydroxyphenones with 1,1-dichloroethylene generates the corresponding chloromethylene furans. These labile intermediates undergo a facile rearrangement into benzofuran carbaldehydes under mild acidic conditions.
Polymer bromide-DMSO: Novel reagent system for the oxidation of alcohols to carbonyl compounds
Prasanna,Mohanaraju
experimental part, p. 6971 - 6973 (2012/02/13)
A novel method for the oxidation of alcohols to aldehydes is described using polymer bromide-DMSO at room temperature. The condition described enables clean and fast conversion to desired carbonyl compounds and a broad range of substrates are tolerated. The resin recovery and recyclability make the protocol more ecofriendly.
Synthesis of aryl ketones by palladium(II)-catalyzed decarboxylative addition of benzoic acids to nitriles
Lindh, Jonas,Sjoeberg, Per J. R.,Larhed, Mats
supporting information; experimental part, p. 7733 - 7737 (2011/01/05)
An efficient, sustainable method for the preparation of aryl ketones from ortho-substituted benzoic acids proceeds through their decarboxylation to generate an aryl-palladium species, followed by addition to a nitrile and hydrolysis of the intermediate ketimine.
Aerobic oxidation of benzylic halides to carbonyl compounds with molecular oxygen catalyzed by tempo/kno2 in aqueous media
Liu, Qifa,Lu, Ming,Yang, Fei,Wei, Wei,Sun, Feng,Yang, Zhenbang,Huang, Sufeng
scheme or table, p. 1106 - 1114 (2010/04/29)
Benzylic halides were successfully oxidized to the corresponding aldehydes and ketones in good to excellent yields in aqueous media with molecular oxygen as oxidant in the presence of catalytic amounts of TEMPO (2,2,6,6- tetramethylpiperidyl-1-oxy) and potassium nitrite (KNO2).
THERAPEUTIC AGENTS, AND METHODS OF MAKING AND USING THE SAME
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Page/Page column 58; 99-100, (2008/06/13)
In part, the present invention is directed towards compounds with FabI inhibiting properties. Such compounds may also inhibit other enzymes, including those similar to FabI either structurally or functionally, for example, Fab K. Kits and compositions that include the disclosed compounds are also provided. Methods of treating a subject with a bacterial illness is also disclosed.
