Month: October 2022

On November 13, 2014, Hirasawa, Hideaki; Kawamura, Naohiro; Kobayashi, Junichi published a patent.Product Details of 1459793-02-2 The title of the patent was Preparation of α-substituted glycine amides as TRPM8 inhibitors. And the patent contained the following:

Title compounds I [A1 = C6-10 aryl (optionally substituted with halo, hydroxy, C1-6 alkyl, etc.), 5-membered heterocyclyl (optionally substituted with halo, hydroxy, C1-6 alkyl, etc.) or 6-membered heterocyclyl (optionally substituted with halo, hydroxy, C1-6 alkyl, etc.); A2 = C6-10 aryl (optionally substituted with halo, hydroxy, C1-6 alkyl, etc.), heterocyclyl (optionally substituted with halo, hydroxy, C1-6 alkyl, etc.) or C3-6 cycloalkyl; X = CH or N; Y = -CR1R2- or oxygen atom; R1, R2 = independently H, halo or C1-6 alkyl; R3, R4 = independently H, halo, C1-6 alkyl, etc.; n = 1 or 2; or pharmacol. acceptable salts thereof] were prepared For example, to a solution of (R)-4,6-difluoroindan-1-ylamine (0.1 g) in methanol (1 mL) was added benzaldehyde (0.063 g), the resulting mixture was stirred at 60° for 1 h, treated with nicotinic acid (0.073 g) and 4-phenylcyclohexen-1-ylisocyanide (0.108 g) [room temperature → 60° (overnight)], cooled to room temperature, concentrated in vacuo, and treated with THF (3 mL), water (12 μL) and HCl (4 mol/L in dioxane, 440 μL) at room temperature for 1.5 h to give, after work-up, compound II (0.076 g). The invention compounds showed potent inhibitory effect on icilin-induced wet-dog shaking in rat. Compounds I are claimed useful for the treatment of diseases or conditions associated with afferent nerve hyperexcitability or injury. The experimental process involved the reaction of (S)-2,3-Dihydrobenzofuran-3-amine hydrochloride(cas: 1459793-02-2).Product Details of 1459793-02-2

The Article related to glycine amide preparation trpm8 inhibitor, nerve hyperexcitability disease treatment glycine amide trpm8 inhibition, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Benzocyclopropenes, Benzocyclobutenes, and Indenes and other aspects.Product Details of 1459793-02-2

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

On May 5, 2017, Zhai, Yuntong; Chen, Xiaofei; Zhou, Wei; Fan, Mengyang; Lai, Yisheng; Ma, Dawei published an article.Related Products of 60770-67-4 The title of the article was Copper-Catalyzed Diaryl Ether Formation from (Hetero)aryl Halides at Low Catalytic Loadings. And the article contained the following:

Diaryl formation is achieved by coupling phenols and (hetero)aryl halides under the catalysis of CuI/N,N’-bis(2-phenylphenyl) oxalamide (BPPO) or CuI/N-(2-phenylphenyl)-N’-benzyl oxalamide (PPBO) at 90 °C using DMF or MeCN as the solvent. Only 0.2-2 mol % CuI and ligand are required for complete conversion, which represents the lowest catalytic loadings for a general Cu/ligand-catalyzed diaryl ether formation. The experimental process involved the reaction of 5-Iodobenzofuran(cas: 60770-67-4).Related Products of 60770-67-4

The Article related to phenol aryl heteroaryl bromide iodide copper oxalamide catalyzed coupling, diaryl ether preparation, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Ethers, Sulfides, and The Corresponding Onium Compounds and other aspects.Related Products of 60770-67-4

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

On July 15, 2022, Gravatt, Christopher S.; Johannes, Jeffrey W.; King, Eric R.; Ghosh, Avipsa published an article.Electric Literature of 60770-67-4 The title of the article was Photoredox-Mediated, Nickel-Catalyzed Trifluoromethylthiolation of Aryl and Heteroaryl Iodides. And the article contained the following:

Herein, a method employing a bench-stable Ni(II) salt and an iridium photocatalyst that was mediated the trifluoromethylthiolation of a wide range of electronically diverse aryl and heteroaryl iodides, likely via a Ni(I)/Ni(III) catalytic cycle was reported. The reaction was broad functional group tolerance and potential for application in medicinal chem., as demonstrated by a late-stage functionalization approach to access (racemic)-Monepantel. The experimental process involved the reaction of 5-Iodobenzofuran(cas: 60770-67-4).Electric Literature of 60770-67-4

The Article related to aryl iodide silver trifluoromethanethiolate nickel iridium photochem trifluoromethylthiolation, trifluoromethyl thioarene preparation, racemic monepantel preparation, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Ethers, Sulfides, and The Corresponding Onium Compounds and other aspects.Electric Literature of 60770-67-4

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

On June 30, 1988, Redondo, Jordi; Sanchez-Ferrando, Francisco; Valls, Montserrat; Virgili, Albert published an article.Electric Literature of 53724-96-2 The title of the article was Selective heteronuclear NOE enhancements in benzoheterocycles. Effect of ring size on indirect three-spin effects. And the article contained the following:

The 80 MHz 1H NMR and 20 MHz 13C NMR spectra of 5 4-methylcoumarins, 6 4-methyl-2(1H)-quinolones and 9 3-methylbenzo[b]furans, including 6 new compounds, were fully assigned. Homonuclear 1H〈1H〉 NOEs and selective heteronuclear 13C〈1H〉 NOEs were measured after low-power pre-saturation of the Me protons. Indirect, neg. heteronuclear NOE enhancements were found in suitable 3-spin systems of the 13C-1H-〈1H〉 type, and their magnitude was dependent on ring size. The 1st examples of indirect, heteronuclear NOE enhancements on non-protonated carbons are described. The experimental process involved the reaction of Ethyl 6-methoxy-3-methylbenzofuran-2-carboxylate(cas: 53724-96-2).Electric Literature of 53724-96-2

The Article related to benzoheterocycle noe heteronuclear, nmr benzoheterocycle, Physical Organic Chemistry: Resonance Spectra (Electron Spin, Nuclear Magnetic and Fourier Transform Nuclear Magnetic, Quadrupole, etc.) and other aspects.Electric Literature of 53724-96-2

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

On March 8, 2021, Liu, Jiandong; Gong, Hegui; Zhu, Shaolin published an article.Synthetic Route of 60770-67-4 The title of the article was BH3·Me2S: An Alternative Hydride Source for NiH-Catalyzed Reductive Migratory Hydroarylation and Hydroalkenylation of Alkenes. And the article contained the following:

Borane dimethylsulfide (BMS) was found to be an efficient hydride source for nickel-hydride catalyzed reductive migratory hydrofunctionalization reactions. Catalytic reductive migratory hydroarylation and migratory hydroalkenylation were achieved with BMS in high yields and with excellent regioselectivity. A large-scale experiment employing as little as 0.5 equiv of BH3·Me2S as the hydride source delivered the desired migratory hydroarylation product in high yield and selectivity. The experimental process involved the reaction of 5-Iodobenzofuran(cas: 60770-67-4).Synthetic Route of 60770-67-4

The Article related to arylalkane preparation, nickel catalyst regioselective hydroarylation aryl alkene iodoarene bromoarene, bromoalkene regioselective hydroarylation aryl alkene nickel catalyst and other aspects.Synthetic Route of 60770-67-4

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

On December 31, 2019, Cai, Zhong-Jian; Liu, Chen-Xu; Wang, Qiang; Gu, Qing; You, Shu-Li published an article.Application In Synthesis of 5-Iodobenzofuran The title of the article was Thioketone-directed rhodium(I) catalyzed enantioselective C-H bond arylation of ferrocenes. And the article contained the following:

Planar chiral ferrocenes have received great attention in both academia and industry. Although remarkable progresses have been made over the past decade, the development of efficient and straightforward methods for the synthesis of enantiopure planar chiral ferrocenes remains highly challenging. Herein, authors report a rhodium(I)/phosphonite catalyzed thioketone-directed enantioselective C-H bond arylation of ferrocenes. Readily available aryl iodides are used as the coupling partners in this transformation, leading to a series of planar chiral ferrocenes in good yields and excellent enantioselectivities (up to 86% yield, 99% ee). Of particular note, heteroaryl coupled ferrocenes, which are difficult to access with previous approaches, can be obtained in satisfactory results. The experimental process involved the reaction of 5-Iodobenzofuran(cas: 60770-67-4).Application In Synthesis of 5-Iodobenzofuran

The Article related to thioketone rhodium phosphonite catalyzed enantioselective carbon hydrogen arylation ferrocene, aryl thioketone ferrocene complex preparation crystal mol structure reactivity and other aspects.Application In Synthesis of 5-Iodobenzofuran

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

On September 23, 2022, Zhang, Yan; Liu, Wen; Xu, Yuenian; Liu, Yong; Peng, Jiajian; Wang, Minyan; Bai, Ying; Lu, Hua; Shi, Zhuangzhi; Shao, Xinxin published an article.Electric Literature of 60770-67-4 The title of the article was S-(Methyl-d3) Arylsulfonothioates: A Family of Robust, Shelf-stable, and Easily Scalable Reagents for Direct Trideuteromethylthiolation. And the article contained the following:

A family of electrophilic deuterated methylthiolating reagents, S-(Methyl-d3) arylsulfonothioates, was developed in two or three steps from cheap d4-MeOH in high yields. S-(Methyl-d3) arylsulfonothioates represent a kind of powerful deuterated methylthiolating reagent and allow modular (trideuteromethyl)thiolation with a variety of nucleophiles or electrophiles including aryl(hetero) iodides, boronic acids esters, terminal alkynes, β-ketoester, and oxindole under mild reaction conditions. A structure-reactivity research study was conducted and provided a new avenue for the development of deuterated methylthiolating reagents and efficient methodol. for (trideuteromethyl)thiolation. The experimental process involved the reaction of 5-Iodobenzofuran(cas: 60770-67-4).Electric Literature of 60770-67-4

The Article related to structure reactivity trideuteromethylthiolation trideuteromethyl arylsulfonothioate, trideuteromethyl arylsulfonothioate preparation methylthiolation nucleophile electrophile and other aspects.Electric Literature of 60770-67-4

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Kusy, Rafal; Lindner, Marcin; Wagner, Jakub; Grela, Karol published an article in 2021, the title of the article was Highly functional group tolerant, (E)-selective transfer semihydrogenation of alkynes catalyzed by iridium complex bearing unsymmetrical ferrocene-based phosphine ligand.Product Details of 60770-67-4 And the article contains the following content:

Herein, authors present (E)-selective transfer semihydrogenation of alkynes based on in situ generated iridium complex from [Ir(COD)Cl]2 and unsym. ferrocene-based phosphine ligand in the presence of formic acid as a hydrogen donor. The catalytic system is distinguished by unprecedented chemoselectivity and exceptional stereoselectivity substantiated by the broad scope of tested substrates, including natural products derivatives The uniform reaction conditions may be applied to various alkynes, owing to a lack of over-reduction The intriguing difference in catalytic activity between unsym. and sym. ferrocene-based ligands was attributed to divergent coordination and steric hindrance. The presented methodol. constitutes a solution to the common limitations of the published catalytic systems. The experimental process involved the reaction of 5-Iodobenzofuran(cas: 60770-67-4).Product Details of 60770-67-4

The Article related to ferrocenyl diphosphine iridium catalyzed stereoselective chemoselective transfer semihydrogenation alkyne, crystal mol structure ferrocenyl diphosphine iridium cyclooctadiene complex and other aspects.Product Details of 60770-67-4

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

On September 1, 2018, Wang, Shuxiang; Li, Bo; Liu, Bo; Huang, Min; Li, Deyi; Guan, Lihong; Zang, Jie; Liu, Dan; Zhao, Linxiang published an article.COA of Formula: C13H14O4 The title of the article was Design and synthesis of novel 6-hydroxy-4-methoxy-3-methylbenzofuran-7-carboxamide derivatives as potent Mnks inhibitors by fragment-based drug design. And the article contained the following:

A novel series of 6-hydroxy-4-methoxy-3-methylbenzofuran-7-carboxamide derivatives featured with various C-2 substituents were designed and synthesized as Mnks inhibitors through fragment-based drug design. Among them, 5b, 5i, 5o and 8k showed the best Mnk2 inhibitory activity with IC50 values of 1.45, 1.16, 3.55 and 0.27 μM, resp. And these compounds inhibited the activity of Mnk1 at the same time. Furthermore, compounds 5o and 8k exhibited anti-proliferative effects to human leukemia cancer THP-1 and MOLM-13 cell lines and colon cancer HCT-116 cell line. Moreover, Western blot assay suggested that 8k could decrease the levels of p-eIF4E in a dose-dependent manner in HCT-116 cells. Docking studies demonstrated strong interactions between 8k and Mnk2. Therefore, this unique benzofuran scaffold demonstrated great potential to be further explored as potent Mnks inhibitors with improved potency. The experimental process involved the reaction of Ethyl 6-methoxy-3-methylbenzofuran-2-carboxylate(cas: 53724-96-2).COA of Formula: C13H14O4

The Article related to benzofuran synthesis antitumor mnk kinase leukemia, 6-hydroxy-4-methoxy-3-methylbenzofuran-7-carboxamide derivatives, anti-proliferative effects, fragment-based drug design, mnks inhibitors and other aspects.COA of Formula: C13H14O4

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

On March 15, 2019, Gao, Mengyu; Sun, Deli; Gong, Hegui published an article.Quality Control of 5-Iodobenzofuran The title of the article was Ni-Catalyzed Reductive C-O Bond Arylation of Oxalates Derived from α-Hydroxy Esters with Aryl Halides. And the article contained the following:

A Ni-catalyzed reductive cross-coupling of α-hydroxycarbonyl compounds modified with oxalyl groups and aryl halides has been developed that furnishes α-aryl esters under mild conditions and tolerates a variety of functionalized aryl halides bearing electron-withdrawing and -donating groups. This work highlights C-O bond fragmentation on secondary alkyl carbon centers that generates α-carbonyl radicals. The experimental process involved the reaction of 5-Iodobenzofuran(cas: 60770-67-4).Quality Control of 5-Iodobenzofuran

The Article related to synthesis aryl ester reductive cross coupling oxalate aryl halide, aryl ester preparation arylation aryl halide oxalate radical fragmentation, oxalate radical fragmentation reduction potential and other aspects.Quality Control of 5-Iodobenzofuran

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem