Tag: 100-200

A novel ¹⁸F-labeled pyridyl benzofuran derivative for imaging of β-amyloid plaques in Alzheimer’s brains was written by Cheng, Yan;Ono, Masahiro;Kimura, Hiroyuki;Kagawa, Shinya;Nishii, Ryuichi;Saji, Hideo. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2010.Recommanded Product: (5-Methoxybenzofuran-2-yl)boronic acid This article mentions the following:

A potential probe for PET targeting β-amyloid plaques in Alzheimer’s disease (AD) brain, FPYBF-1 (5-(5-(2-(2-(2-fluoroethoxy)ethoxy)ethoxy)benzofuran-2-yl)-N,N-dimethylpyridin-2-amine), was synthesized and evaluated. In experiments in vitro, FPYBF-1 displayed high affinity for Aβ(1-42) aggregates (K _i = 0.9 nM), and substantial labeling of β-amyloid plaques in sections of postmortem AD brains but not control brains. In experiments in vivo, [¹⁸F]FPYBF-1 displayed good initial uptake (5.16%ID/g at 2 min postinjection) and rapid washout from the brain (2.44%ID/g at 60 min postinjection) in normal mice, and excellent binding to β-amyloid plaques in a murine model of AD. Furthermore, the specific labeling of plaques labeling was observed in autoradiographs of autopsied AD brain sections. [¹⁸F]FPYBF-1 may be a useful probe for imaging β-amyloid plaques in living brain tissue. In the experiment, the researchers used many compounds, for example, (5-Methoxybenzofuran-2-yl)boronic acid (cas: 551001-79-7Recommanded Product: (5-Methoxybenzofuran-2-yl)boronic acid).

(5-Methoxybenzofuran-2-yl)boronic acid (cas: 551001-79-7) belongs to benzofurans derivatives. Benzofuran is the “”parent”” of many related compounds with more complex structures. For example, psoralen is a benzofuran derivative that occurs in several plants. Introduction of benzofurans in organic synthesis, particularly drug synthesis, involves generally the use of their metalated species as nucleophiles in addition reactions or in metal-catalysed cross-coupling reactions.Recommanded Product: (5-Methoxybenzofuran-2-yl)boronic acid

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Ligand-Promoted Nickel-Catalyzed para-Selective Carboxylation of Anisoles was written by Tu, Guangliang;Ju, Guodong;Ji, Shun-Jun;Zhao, Yingsheng. And the article was included in Organic Letters in 2022.Category: benzofurans This article mentions the following:

It has always been a challenge in free radical chem. to control site selectivity during the reaction of free radicals with aromatic rings. Herein, the site-selective carboxylation of anisoles through the direct reaction of the bromoform radical with a benzene ring at the para position under the assistance of 2,9-dimethyl-4,7-diphenyl-1,10-phenanthroline with nickel(II) as the catalyst is reported. A wide variety of anisoles were compatible, leading to para-carboxylated products in moderate to good yields. A preliminary mechanistic study suggested that the Ni(II) complex coordinates with the methoxyl group of the aromatic ring, which may have increased the steric hindrance at the ortho and meta positions, while this weak interaction reduces the aromaticity of the aromatic ring, affording an activated Ph ring, thereby leading to highly para-selective carboxylation. In the experiment, the researchers used many compounds, for example, Methyl benzofuran-2-carboxylate (cas: 1646-27-1Category: benzofurans).

Methyl benzofuran-2-carboxylate (cas: 1646-27-1) belongs to benzofurans derivatives. Benzofurans are only weakly aromatic in nature and they are cleaved by many oxidative and reductive conditions. Benzofurans have also made significant and distinctive contributions to biology. They exhibit several biological activities that range from antiviral, antimicrobial, antitumor, anti-inflammatory.Category: benzofurans

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Scaffold hopping and optimisation of 3′,4′-dihydroxyphenyl- containing thienopyrimidinones: synthesis of quinazolinone derivatives as novel allosteric inhibitors of HIV-1 reverse transcriptase-associated ribonuclease H was written by Tocco, Graziella;Esposito, Francesca;Caboni, Pierluigi;Laus, Antonio;Beutler, John A.;Wilson, Jennifer A.;Corona, Angela;Le Grice, Stuart F. J.;Tramontano, Enzo. And the article was included in Journal of Enzyme Inhibition and Medicinal Chemistry in 2020.Application In Synthesis of 3-Aminobenzofuran-2-carboxamide This article mentions the following:

Bioisosteric replacement and scaffold hopping are powerful strategies in drug design useful for rationally modifying a hit compound towards novel lead therapeutic agents. Recently, we reported a series of thienopyrimidinones that compromise dynamics at the p66/p51 HIV-1 reverse transcriptase (RT)-associated RNase H (RNase H) dimer interface, thereby allosterically interrupting catalysis by altering the active site geometry. Although they exhibited good submicromolar activity, the isosteric replacement of the thiophene ring, a potential toxicophore, is warranted. Thus, in this article, the most active 2-(3,4-dihydroxyphenyl)-5,6-dimethylthieno[2,3-d]pyrimidin-4(3H)-one was selected as the hit scaffold and several isosteric substitutions of the thiophene ring were performed. A novel series of highly active RNase H allosteric quinazolinone inhibitors was thus obtained. To determine their target selectivity, they were tested against RT-associated RNA-dependent DNA polymerase (RDDP) and integrase (IN). Interestingly, none of the compounds were particularly active on (RDDP) but many displayed micromolar to submicromolar activity against IN. In the experiment, the researchers used many compounds, for example, 3-Aminobenzofuran-2-carboxamide (cas: 54802-10-7Application In Synthesis of 3-Aminobenzofuran-2-carboxamide).

3-Aminobenzofuran-2-carboxamide (cas: 54802-10-7) belongs to benzofurans derivatives.Benzofuran is one of the most significant oxygen-containing heterocycles consisting of fused benzene and furan ring, which are widely presented in various naturally occurring and synthetically active compounds. Benzofurans are stable towards alkali and readily polymerize on treatment with sulfuric acid, due to which they are useful for the preparation of low cost chemically relatively inert resins.Application In Synthesis of 3-Aminobenzofuran-2-carboxamide

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

The organocatalytic three-step total synthesis of (+)-frondosin B was written by Reiter, Maud;Torssell, Staffan;Lee, Sandra;MacMillan, David W. C.. And the article was included in Chemical Science in 2010.Related Products of 551001-79-7 This article mentions the following:

The frondosins are a family of marine sesquiterpenes isolated from the sponge Dysidea frondosa that exhibit biol. activities ranging from anti-inflammatory properties to potential application in anticancer and HIV therapy (no biol. testing data presented). A concise enantioselective total synthesis of (+)-frondosin B (I) was described which required a total of three chem. steps. The enantioselective conjugate addition of a benzofuran-derived boronic acid to crotonaldehyde in the presence of an imidazolidinone organocatalyst constructed the critical stereogenic center of frondosin B in the first operation, while the remaining two ring systems of this natural product were installed in the two subsequent steps. A combination of X-ray crystallog. data, deuterium labeling, and chem. correlation studies provides further evidence as to the correct absolute stereochem. assignment of (R) to (+)-frondosin B. In the experiment, the researchers used many compounds, for example, (5-Methoxybenzofuran-2-yl)boronic acid (cas: 551001-79-7Related Products of 551001-79-7).

(5-Methoxybenzofuran-2-yl)boronic acid (cas: 551001-79-7) belongs to benzofurans derivatives. Benzofurans are only weakly aromatic in nature and they are cleaved by many oxidative and reductive conditions. Introduction of benzofurans in organic synthesis, particularly drug synthesis, involves generally the use of their metalated species as nucleophiles in addition reactions or in metal-catalysed cross-coupling reactions.Related Products of 551001-79-7

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Alkaline hydrolysis of the methyl esters of benzo[b]furan-2- and 3-carboxylic acid, benzo[b]thiophene-2- and 3-carboxylic acid, and indole-2- and 3-carboxylic acid was written by Feinstein, A.;Gore, Peter H.;Reed, George Leonard. And the article was included in Journal of the Chemical Society [Section] B: Physical Organic in 1969.Electric Literature of C10H8O3 This article mentions the following:

The rates of alk. hydrolysis of carboxylic acid Me esters, in 70% dioxane follow the sequence 3-benzo[b]furyl >2-benzo[b]furyl >2-benzo[b]thienyl > indol-2-yl > indol-3-yl > phenyl > 3-benzo[b]thienyl. The effect of benzosubstitution on the rates of hydrolysis was determined for furan, thiophene, and pyrrole esters; it ranges from a rate enhancement of ∼200 (for pyrrol-2-yl) to a 70% rate reduction (for 3-thienyl). In the experiment, the researchers used many compounds, for example, Methyl benzofuran-2-carboxylate (cas: 1646-27-1Electric Literature of C10H8O3).

Methyl benzofuran-2-carboxylate (cas: 1646-27-1) belongs to benzofurans derivatives. Benzofurans are only weakly aromatic in nature and they are cleaved by many oxidative and reductive conditions. Substituted benzofurans find applications such as fluorescent sensors, oxidants, in drug discovery, and in another field of chemistry and agriculture.Electric Literature of C10H8O3

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Reductive 3-Silylation of Benzofuran Derivatives via Coupling Reaction with Chlorotrialkylsilane was written by Zheng, Suhua;Zhang, Tianyuan;Maekawa, Hirofumi. And the article was included in Journal of Organic Chemistry in 2020.Product Details of 1646-27-1 This article mentions the following:

Reductive silylation of benzofurans with an electron-withdrawing group by a magnesium metal and the subsequent oxidative rearomatization by DDQ gave the selective formation of less reported 3-silylated benzofurans in moderate to good yields under mild reaction conditions with wide substituent scope. The silyl group introduced on the five-membered ring by the reductive coupling could survive with no elimination throughout the oxidation process. The silylated heteroaromatic skeleton is useful as an intermediate in organic synthesis, and its practical utility was also demonstrated by several transformation reactions. In the experiment, the researchers used many compounds, for example, Methyl benzofuran-2-carboxylate (cas: 1646-27-1Product Details of 1646-27-1).

Methyl benzofuran-2-carboxylate (cas: 1646-27-1) belongs to benzofurans derivatives. Benzofurans are compounds with a planar structure having 10 pi electrons that include the lone pair on oxygen atom, which makes it more susceptible to electrophilic attack. As benzofurans are prone to undergo ring opening of the heterocycle, examples of reduction of this type of aromatics by using dissolving metals are rather scarce.Product Details of 1646-27-1

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Identification of 3-aminothieno[2,3-b]pyridine-2-carboxamides and 4-aminobenzothieno[3,2-d]pyrimidines as LIMK1 inhibitors was written by Sleebs, Brad E.;Levit, Alla;Street, Ian P.;Falk, Hendrik;Hammonds, Tim;Wong, Ai Ching;Charles, Mark D.;Olson, Michael F.;Baell, Jonathan B.. And the article was included in MedChemComm in 2011.Computed Properties of C9H8N2O2 This article mentions the following:

A high throughput chem. screening campaign has led to the identification of 3-aminobenzo[b]thiophene-2-carboxamides as LIMK1 inhibitors. Evolution of bicyclic hits to the tricyclic 4-aminobenzothieno[3,2-d]pyrimidine, using a traditional medicinal chem. SAR guided approach, resulted in a significant increase in potency. Further elaboration has seen the 7-phenyl-4-aminobenzothieno[3,2-d]pyrimidine emerge as a LIMK1 inhibitor lead candidate. In the experiment, the researchers used many compounds, for example, 3-Aminobenzofuran-2-carboxamide (cas: 54802-10-7Computed Properties of C9H8N2O2).

3-Aminobenzofuran-2-carboxamide (cas: 54802-10-7) belongs to benzofurans derivatives. Benzofurans are only weakly aromatic in nature and they are cleaved by many oxidative and reductive conditions. Benzofurans are stable towards alkali and readily polymerize on treatment with sulfuric acid, due to which they are useful for the preparation of low cost chemically relatively inert resins.Computed Properties of C9H8N2O2

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Fluorescent Sensor for Sequentially Monitoring Zinc(II) and Cyanide Anion in Near-Perfect Aqueous Media was written by Jang, Hyo Jung;Kang, Ji Hye;Lee, Misun;Lim, Mi Hee;Kim, Cheal. And the article was included in Industrial & Engineering Chemistry Research in 2018.Application of 54802-10-7 This article mentions the following:

The authors report a sensor, I, for sequentially detecting Zn²⁺ and CN^– based on fluorescence. Sensor I was prepared through the reaction of 3-aminobenzofuran-2-carboxamide with 4-diethylaminosalicylaldehyde. Sensor I1 showed a selective off-on fluorescent response toward Zn²⁺, distinguishing Zn²⁺ from Cd²⁺. The limit of I (0.35 μM) for monitoring Zn²⁺ is lower than the World Health Organization (WHO) guideline (76 μM) for water available for drinking. Importantly, sensor I could sense Zn²⁺ in living cells and aqueous media. The resulting I-Zn²⁺ complex functioned as an efficient on-off sensor for CN^–. The mechanisms of I for detecting Zn²⁺ and CN^– were explained by spectroscopic, spectrometric, and theor. studies. In the experiment, the researchers used many compounds, for example, 3-Aminobenzofuran-2-carboxamide (cas: 54802-10-7Application of 54802-10-7).

3-Aminobenzofuran-2-carboxamide (cas: 54802-10-7) belongs to benzofurans derivatives. Many natural or synthetic compounds containing benzofuran skeletons have been found to possess remarkable activity as agrochemicals and pharmaceuticals. They are also prone to polymerisation in the presence of concentrated mineral acids and Lewis acids.Application of 54802-10-7

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Microwave-Assisted N-Allylation/Homoallylation-RCM Approach: Access to Pyrrole-, Pyridine-, or Azepine-Appended (Het)aryl Aminoamides was written by Novanna, Motakatla;Kannadasan, Sathananthan;Shanmugam, Ponnusamy. And the article was included in ACS Omega in 2020.Computed Properties of C9H8N2O2 This article mentions the following:

A facile and diversity-oriented approach was developed for the synthesis of pyrrole-, pyridine-, or azepine-appended (het)aryl aminoamides via the N-allylation/homoallylation-ring-closing metathesis (RCM) strategy. Microwave condition was efficiently utilized for N-allylation of (het)aryl aminoamides to synthesized di-, tri-, and tetra-allyl/homoallylated RCM substrates in good yields. All of the RCM substrates were successfully converted to resp. pyrroles, pyridines and azepines via RCM. All of the five-, six-, and seven-membered N-heterocycles were synthesized in shorter reaction times with excellent yields without isomerization products. A one-pot reaction to synthesized pyrroles without isolating corresponding RCM substrates was achieved successfully. The synthetic utility of the compoundpyrroles was demonstrated by synthesizing biaryl derivatives pyrroles under the microwave Suzuki coupling reaction condition. In the experiment, the researchers used many compounds, for example, 3-Aminobenzofuran-2-carboxamide (cas: 54802-10-7Computed Properties of C9H8N2O2).

3-Aminobenzofuran-2-carboxamide (cas: 54802-10-7) belongs to benzofurans derivatives. Benzofuran derivatives have shown many biological activities, including antifungal and antimicrobial properties, and acting as antagonists of H3 receptors and angiotensin II. They are also prone to polymerisation in the presence of concentrated mineral acids and Lewis acids.Computed Properties of C9H8N2O2

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Synthesis, characterization, antibacterial and anthelmintic activities of copper(II) complexes with benzofuran schiff bases was written by Reddy, K. Ramakrishna;Reddy, K. Madhusudan;Mahendra, K. N.. And the article was included in Indian Journal of Chemistry, Section A: Inorganic, Bio-inorganic, Physical, Theoretical & Analytical Chemistry in 2006.Electric Literature of C9H8N2O2 This article mentions the following:

Cu(II)chloride reacts with Schiff bases derived from benzaldehydes/acetophenone with 3-amino-2-benzofuran carboxamide or ethyl-3-amino-2-benzofuran carboxylate to yield polymeric complexes CuLCl₂ (L = Schiff base). The authenticity of the ligands and their complexes was established by micro anal., magnetic susceptibility, IR, electronic, ESR spectral studies and elec. conductance measurements. The ligands act as bidentate, with azomethane N and carbonyl O atom as donor sites. Probably Cu(II) complexes are polymeric with octahedral geometries. All the ligands and their metal complexes were screened for antibacterial activity against two bacteria, viz. S.aureus and E.coli. Several complexes show promising results against S.aureus. Anthelmintic activity of the ligands and the complexes was tested on earthworms. The activity is enhanced significantly on complexation. In the experiment, the researchers used many compounds, for example, 3-Aminobenzofuran-2-carboxamide (cas: 54802-10-7Electric Literature of C9H8N2O2).

3-Aminobenzofuran-2-carboxamide (cas: 54802-10-7) belongs to benzofurans derivatives. Many natural or synthetic compounds containing benzofuran skeletons have been found to possess remarkable activity as agrochemicals and pharmaceuticals. As benzofurans are prone to undergo ring opening of the heterocycle, examples of reduction of this type of aromatics by using dissolving metals are rather scarce.Electric Literature of C9H8N2O2

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem