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In this paper we wish to report on a variety of expedient chemical transformations and purifications achieved via a generic ‘catch and release’ methodology, based on a synthetically inert bipyridyl chelating tag that can be selectively captured with a resin-bound copper(II) species. Utilising this approach we are able to derive many of the same benefits associated with both solid phase synthesis and supported reagent methods. The Royal Society of Chemistry 2005.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H1048O – PubChem

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The present invention provides a novel benzamide derivative represented by formula 1 and an isomer, a pharmaceutically acceptable salt or hydrate thereof, and a composition for activating a 5-HT4 receptor comprising the same, as an active ingredient. Benzamide derivatives of the present invention has superior affinity for 5-HT4 receptors, capability to reduce the gastric evacuation time, capability to alleviate ventricular tachycardia, ventricular fibrillation, torsades de pointes and QT prolongation, and low toxicity. Therefore, benzamide derivatives of the present invention are therapeutically effective for digestive system diseases.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H717O – PubChem

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Memoquin (1) is a lead compound multitargeted against Alzheimer’s disease (AD). It is an AChE inhibitor, free-radical scavenger, and inhibitor of amyloid-beta (Abeta) aggregation. A new series of 1 derivatives was designed and synthesized by linking its 2,5-diamino-benzoquinone core with motifs that are present in the structure of known amyloid binding agents like curcumin, the benzofuran derivative SKF64346, or the benzothiazole bearing compounds KHG21834 and BTA-1. The weaker AChE inhibitory potencies and the concomitant nearly equipotent anti-amyloid activities of the new compounds with respect to 1 resulted in a more balanced biological profile against both targets. Selected compounds turned out to be effective Abeta aggregation inhibitors in a cell-based assay. By properly combining two or more distinct pharmacological properties in a molecule, we can achieve greater effectiveness compared to single-targeted drugs for investigating AD.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H751O – PubChem

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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 4265-16-1, name is Benzo[b]furan-2-carboxaldehyde, introducing its new discovery. SDS of cas: 4265-16-1

A palladium catalyst in combination with two types of phosphine ligands efficiently catalyzes direct C-H alkylation of heteroarenes with secondary and tertiary alkyl bromides under irradiation conditions. Irradiation of blue light-emitting diodes (blue LEDs) effectively excites phosphine-ligated palladium catalyst to facilitate oxidative addition with alkyl bromides, and also excites the alkylpalladium species to enable the generation of alkyl radicals to react with heteroarenes.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H1095O – PubChem

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Background: Drug resistance and reservoirs of latent viral infection have prevented total eradication of the HIV-virus which underlines the need for continuous efforts in the discovery of new anti-HIV agents. The present study deals with the synthesis of novel compounds based on naturally occurring scaffolds and their evaluation as potential anti-HIV agents. Objective: Design and synthesis of styrylquinoline scaffold based new molecules and evaluation of their anti-HIV-1 activity. Methods: A series of forty three new styrylquinolines (SQLs) was designed and synthesized. The newly synthesized compounds were tested for anti-HIV-1 activity against HIV-1VB59 and HIV-1UG070 primary isolates in TZM-bl cell lines. Results: The most active compounds 9 and 34 (IC50 = 0.5-4.0 muM), also exhibited significant inhibition activity against HIV-1VB51 primary isolate in PBMCs (IC50 = 7.3 muM). Compounds 9 and 34 were also found to inhibit HIV-1 entry into host cells and fusion inhibitory activities. The study encourages further exploration of SQL nucleus to design anti-HIV-1 agents. Conclusion: The study encourages further exploration of SQL nucleus to design anti-HIV-1 agents.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H937O – PubChem

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Several substituted benzofuryl chalcone analogues were synthesized and by oxidation of these compounds the corresponding 2-benzofurylchromones, 3-hydroxy-2-benzofurylchromones and chalcone epoxides were prepared. 3-Benzofurylchromones were obtained from the chalcone epoxides.According to the (1)H-NMR spectra, analyzed by the LSR technique, it was found that 2-benzofurylchromones exist preferably in the transoid conformation.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H833O – PubChem

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Highly functionalized aldol-type products bearing a beta-quaternary center and a stereoselectively controlled gamma-hydroxy function are readily prepared by the diastereoselective addition of an allylic zinc reagent embedded in an isoxazole ring to various aromatic and heteroaromatic aldehydes, in the presence of Lewis acids, such as MgCl2 or LaCl32 LiCl. After reductive cleavage of the N=O bond by using Fe, NH4Cl, aldol-type products bearing a stereocontrolled beta-quaternary center and a gamma-hydroxy group were observed. The benzylic reactivity of the isoxazolylmethylzinc reagent towards other electrophiles, such as acid chlorides, aryl and allylic halides, as well as aldehydes in the presence of BF3OEt2 are also described. Highly functionalized aldol-type products bearing a beta-quaternary center and a stereoselectively controlled gamma-hydroxy function are readily prepared by the diastereoselective addition of an allylic zinc reagent to various aromatic and heteroaromatic aldehydes in the presence of Lewis acids MgCl2 or LaCl32 LiCl (see scheme).

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H885O – PubChem

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The dual role of the bicyclic amidine base 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) was demonstrated in a synthesis of terminal aryl- and styryl-acetylenes. Mechanistically, a tandem process involving elimination/Umpolung/protonation occurs in a single step to generate terminal aryl- and styryl-acetylenes from geminal dibromoalkenes. The key to the success of this transformation lies in the organobase-mediated generation of the acetylide from the 1-bromoalkynes at room temperature. The unique characteristics of DBU as an inherently safer reagent make it an attractive alternative to previous systems wherein required pyrophoric reagents and nonambient temperatures remain unsolved issues. The procedure does not work for the synthesis of alkyl-acetylenes.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H957O – PubChem

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Inspired by the dicationic nature of the electrophilic fluorinating reagent, Selectfluor (1), we rationally designed a series of dicarboxylic acid precatalysts (2), which, when deprotonated, act as anionic phase-transfer catalysts for asymmetric fluorination of alkenes. Among them, 2a having the shortest linker moiety efficiently catalyzed unprecedented 6-endo-fluoro-cyclization of various allylic amides, affording fluorinated dihydrooxazine compounds with high enantioselectivity (up to 99% ee). In addition to cyclic substrates, acyclic trisubstituted alkenes underwent the reaction with good diastereoselectivity, whereas low diastereoselectivity was observed for linear disubstituted alkenes. Results suggest that the reaction proceeds via a fluoro-carbocation intermediate.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H807O – PubChem

Discovery of Benzo[b]furan-2-carboxaldehyde

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A simple synthesis method of nitriles from corresponding aldehydes by electrochemical oxidation was developed with ammonium acetate as the nitrogen source and 4-acetamido- 2,2,6,6-tetramethylpiperidinyl-l-oxy (4-AcNH-TEMPO) as the catalyst. Cyclic voltammetry was performed to investigate the electrocatalytic activity of 4-AcNH-TEMPO for the conversion of benzaldehyde to benzonitrile. On the basis of in situ FTIR data and cyclic voltammetry experiments, a reaction mechanism, involving the redox of 4-AcNH-TEMPO and the generation of intermediate imine during the reaction, was proposed. This electrocatalytic reaction system provided an efficient protocol for synthesis of aromatic nitriles at room temperature with moderate to high yields.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H1121O – PubChem