Category: 16004-15-2

Recommanded Product: 16004-15-2. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 1-(Bromomethyl)-4-iodobenzene, is researched, Molecular C7H6BrI, CAS is 16004-15-2, about Evolution of a 4-Benzyloxy-benzylamino Chemotype to Provide Efficacious, Potent, and Isoform Selective PPARα Agonists as Leads for Retinal Disorders.

Peroxisome proliferator-activated receptor alpha (PPARα) is expressed in retinal Müller cells, endothelial cells, and in retinal pigment epithelium; agonism of PPARα with genetic or pharmacol. tools ameliorates inflammation, vascular leakage, neurodegeneration, and neovascularization associated with retinal diseases in animal models. As such, PPARα is a promising drug target for diabetic retinopathy and age-related macular degeneration. Herein, we report proof-of-concept in vivo efficacy in an streptozotocin-induced vascular leakage model (rat) and preliminary pharmacokinetic assessment of a first-generation lead 4a (A91). Addnl., we present the design, synthesis, and evaluation of second-generation analogs, which led to the discovery of 4u and related compounds that reach cellular potencies <50 nM and exhibit >2,700-fold selectivity for PPARα over other PPAR isoforms. These studies identify a pipeline of candidates positioned for detailed PK/PD and pre-clin. evaluation.

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Reference:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 1-(Bromomethyl)-4-iodobenzene( cas:16004-15-2 ) is researched.Synthetic Route of C7H6BrI.Yang, Ren-Yin; Gao, Xinyan; Gong, Kehao; Wang, Juan; Zeng, Xiaojun; Wang, Mingwei; Han, Junbin; Xu, Bo published the article 《Synthesis of ArCF2X and [18F]Ar-CF3 via Cleavage of the Trifluoromethylsulfonyl Group》 about this compound( cas:16004-15-2 ) in Organic Letters. Keywords: aryldifluoromethylene compound preparation. Let’s learn more about this compound (cas:16004-15-2).

A versatile synthesis of ArCF2X and [18F]Ar-CF3 type compounds from readily available ArCF2SO2CF3 has been developed. Diverse nucleophiles, including weak nucleophiles such as halides (18F-, Cl-, Br-, and I-), RSH, and ROH, could react with ArCF2SO2CF3 efficiently to give the corresponding difluoromethylene products. The control experiments and the Hammett plot indicated that the reaction might proceed through a difluorocarbocation intermediate generated from the steric hindrance-assisted cleavage of the trifluoromethylsulfonyl group.

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Reference:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: 1-(Bromomethyl)-4-iodobenzene(SMILESS: IC1=CC=C(CBr)C=C1,cas:16004-15-2) is researched.Product Details of 1265884-98-7. The article 《Synthesis and evaluation of new 1-oxa-8-azaspiro[4.5]decane derivatives as candidate radioligands for sigma-1 receptors》 in relation to this compound, is published in Bioorganic & Medicinal Chemistry. Let’s take a look at the latest research on this compound (cas:16004-15-2).

The design, synthesis, and evaluation of a series of 1-oxa-8-azaspiro[4.5]decane I (R = F, I, OCH2CH2F) and 1,5-dioxa-9-azaspiro[5.5]undecane derivatives II (R = F, I, OCH2CH2F, OMe) as selective σ1 receptor ligands has been reported. All seven ligands exhibited nanomolar affinity for σ1 receptors (Ki(σ1) = 0.47 – 12.1 nM) and moderate selectivity over σ2 receptors (Ki(σ2)/ Ki(σ1) = 2 – 44). Compound I (R = OCH2CH2F), with the best selectivity among these ligands, was selected for radiolabeling and further evaluation. Radioligand II (R = OCH2CH2F18) was prepared via nucleophilic 18F-substitution of the corresponding tosylate precursor, with an overall isolated radiochem. yield of 12-35%, a radiochem. purity of greater than 99%, and molar activity of 94 – 121 GBq/μmol. Biodistribution studies of II (R = OCH2CH2F18) in mice demonstrated high initial brain uptake at 2 min. Pretreatment with SA4503 resulted in significantly reduced brain-to-blood ratio (70% – 75% at 30 min). Ex vivo autoradiog. in ICR mice demonstrated high accumulation of the radiotracer in σ1 receptor-rich brain areas. These findings suggest that II (R = OCH2CH2F18) could be a lead compound for further structural modifications to develop potential brain imaging agents for σ1 receptors.

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Reference:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: 1-(Bromomethyl)-4-iodobenzene(SMILESS: IC1=CC=C(CBr)C=C1,cas:16004-15-2) is researched.HPLC of Formula: 60748-47-2. The article 《C(sp3)-H Monoarylation of methanol enabled by a bidentate auxiliary》 in relation to this compound, is published in Organic Letters. Let’s take a look at the latest research on this compound (cas:16004-15-2).

With the assistance of a practical directing group (COAQ), the first catalytic protocol for the palladium-catalyzed C(sp3)-H monoarylation of methanol has been developed, offering an invaluable synthesis means to establish extensive derivatives of crucial arylmethanol functional fragments. Furthermore, the gram-scale reaction, broad substrate scope, excellent functional group compatibility, and even the practical synthesis of medicines further demonstrate the usefulness of this strategy.

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Reference:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Application of 16004-15-2. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 1-(Bromomethyl)-4-iodobenzene, is researched, Molecular C7H6BrI, CAS is 16004-15-2, about External Catalyst-Free Oxidation of Benzyl Halides to Benzoic Acids Using NaOH/TBHP in Water.

An efficient and metal-free methodol. for the oxidation of benzyl halides to benzoic acids using an inexpensive and green oxidant (TBHP) in aqueous basic medium has been developed. This protocol offers an excellent way to avoid adding catalysts and involves the use of an in-situ generated halide ion as catalyst. It is also the first report on the oxidation of benzyl iodides to benzoic acids. A series of carboxylic acids were prepared from benzyl halides in high yields under mild reaction conditions by this method which does not require chromatog. purification Gram scale reactions for the synthesis of the carboxylic acids in good yields have been successfully carried out using benzyl chloride, bromide and iodide. As an industrial application, the synthesis of a key monomer used for the synthesis of polyethylene terephthalate (PET), i. e., terephthalic acid (PTA), has also been accomplished in good yields.

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Reference:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《Silylium-Ion Regeneration by Protodesilylation Enables Friedel-Crafts Alkylation with Less Isomerization and No Defunctionalization》. Authors are He, Tao; Klare, Hendrik F. T.; Oestreich, Martin.The article about the compound:1-(Bromomethyl)-4-iodobenzenecas:16004-15-2,SMILESS:IC1=CC=C(CBr)C=C1).Recommanded Product: 16004-15-2. Through the article, more information about this compound (cas:16004-15-2) is conveyed.

An improved protocol for the Friedel-Crafts alkylation of benzene as well as its methylated and halogenated derivatives with alkyl and benzyl bromides is reported. The reaction is promoted by a counteranion-stabilized silylium ion in the presence of stoichiometric amounts of a simple phenyl-substituted tetraorganosilane. This additive functions as a proton scavenger, regenerating the catalytically active silylium ion through protonation (protodesilylation) by the Wheland intermediate. It is a productive “”proton-into-silylium ion”” generator. The higher proton affinity of silylated compared with alkylated arenes results in fast proton transfer from the Bronsted acidic Wheland intermediate to the ipso position of that phenylsilane, thereby preventing otherwise competing defunctionalization and isomerization at the stage of the Wheland intermediate. The additive was also found to be crucial for turnover in the alkylation with primary alkyl bromides and for the suppression of transbenzylation in the benzylation with more reactive benzyl bromides.

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Reference:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Application of 16004-15-2. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 1-(Bromomethyl)-4-iodobenzene, is researched, Molecular C7H6BrI, CAS is 16004-15-2, about Synthesis and evaluation of thymol-based synthetic derivatives as dual-action inhibitors against different strains of H. pylori and AGS cell line.

Herein, the synthesis of a new series of thymol-based ethers I [R = Me, H2C:CH, CN, EtO2C, Ph, 2-BrC6H4, etc.] and their microbiol. screening against eight strains of H. pylori and the cytotoxic activity against human gastric adenocarcinoma (AGS) cells are reported. Structural anal. comprehended elemental anal. and 1H/13C/19F NMR spectra. The anal. of structure-activity relationships within this mol. library of these structurally-related compounds showed that some chem. modifications of the OH group of thymol led to broad-spectrum growth inhibition on all isolates. Preferred substitutions were benzyl groups compared to alkyl chains and the specific presence of functional groups at para position of the benzyl moiety such as 4-CN and 4-Ph endowed the most anti-H. pylori activity toward all the strains with min. inhibitory concentration (MIC) values up to 4μg/mL. Poly-substitution on the benzyl ring was not essential. Moreover, several compounds characterized by the lowest min. inhibitory concentration/min. bactericidal concentration (MIC/MBC) values against H. pylori were also tested in order to verify a cytotoxic effect against AGS cells with respect to 5-fluorouracil and carvacrol.

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Reference:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Application of 16004-15-2. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 1-(Bromomethyl)-4-iodobenzene, is researched, Molecular C7H6BrI, CAS is 16004-15-2, about Cu-catalyzed N-3-Arylation of Hydantoins Using Diaryliodonium Salts. Author is Neerbye Berntsen, Linn; Nova, Ainara; Wragg, David S.; Sandtorv, Alexander H..

A general Cu-catalyzed, regioselective method for the N-3-arylation of hydantoins I (R = R1 = H, Me, Ph; R2 = H, Me), (R)-5-methylhydantoin and (S)-Tetrahydro-1H-pyrrolo[1,2-c]imidazole-1,3(2H)-dione is described. The protocol utilizes aryl(trimethoxyphenyl)iodonium tosylate [2,4,6-(OCH3)3C6H2IR3]+[4-CH3C6H4SO3]- (R3 = Ph, 2-fluorophenyl, 2,3-dihydro-1-benzofuran-5-yl, etc.) as the arylating agent in the presence of triethylamine and a catalytic amount of a simple Cu-salt. The method is compatible with structurally diverse hydantoins I and operates well with neutral aryl groups or aryl groups bearing weakly donating/withdrawing elements. It is also applicable for the rapid diversification of pharmaceutically relevant hydantoins II [Ar = Ph, 4-(methoxycarbonyl)benzen-1-yl, 4-[(1,3-dioxo-2,3-dihydro-1H-isoindol-2-yl)methyl]benzen-1-yl] and III.

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Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Related Products of 16004-15-2. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: 1-(Bromomethyl)-4-iodobenzene, is researched, Molecular C7H6BrI, CAS is 16004-15-2, about Clustering-Triggered Ultralong Room-Temperature Phosphorescence of Organic Crystals through Halogen-Mediated Molecular Assembly. Author is Sun, Huili; Ding, Riqing; Lv, Shanling; Zhou, Shasha; Guo, Sidan; Qian, Zhaosheng; Feng, Hui.

To achieve efficient room-temperature phosphorescence of organic materials with ultralong lifetime, it is imperative to resolve the dilemma that the introduction of heavy atoms simultaneously improves emission efficiencies and shortens the emission lifetimes. Herein, we report a new mol. design approach for halogenated luminogens with a methylene bridge to avoid the lifetime shortening induced by heavy halogens and propose a general mol. engineering strategy to realize efficient and ultralong room-temperature phosphorescence via halogen-mediated mol. clustering. The halogenated N-benzylcarbazole derivatives show distinct photophys. behaviors depending on different phys. states, including single-mol. state and cluster state. Their crystals demonstrate the halogen-dependent emission duration of room-temperature phosphorescence upon excitation. Exptl. data and theor. anal. indicate that halogen-regulated mol. clustering in the crystal is responsible for the generation of efficient ultralong room-temperature phosphorescence, and halogen-dominated mol. engineering favors the promotion of the intersystem crossing process and the following triplet emissions.

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Reference:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《Silylium-Ion Regeneration by Protodesilylation Enables Friedel-Crafts Alkylation with Less Isomerization and No Defunctionalization》. Authors are He, Tao; Klare, Hendrik F. T.; Oestreich, Martin.The article about the compound:1-(Bromomethyl)-4-iodobenzenecas:16004-15-2,SMILESS:IC1=CC=C(CBr)C=C1).Recommanded Product: 16004-15-2. Through the article, more information about this compound (cas:16004-15-2) is conveyed.

An improved protocol for the Friedel-Crafts alkylation of benzene as well as its methylated and halogenated derivatives with alkyl and benzyl bromides is reported. The reaction is promoted by a counteranion-stabilized silylium ion in the presence of stoichiometric amounts of a simple phenyl-substituted tetraorganosilane. This additive functions as a proton scavenger, regenerating the catalytically active silylium ion through protonation (protodesilylation) by the Wheland intermediate. It is a productive “”proton-into-silylium ion”” generator. The higher proton affinity of silylated compared with alkylated arenes results in fast proton transfer from the Bronsted acidic Wheland intermediate to the ipso position of that phenylsilane, thereby preventing otherwise competing defunctionalization and isomerization at the stage of the Wheland intermediate. The additive was also found to be crucial for turnover in the alkylation with primary alkyl bromides and for the suppression of transbenzylation in the benzylation with more reactive benzyl bromides.

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Reference:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics