Tag: 200-300

On July 31, 2022, Xu, Ying; Chen, Peng; Tang, Lei; Zhang, Xiaojun; Shi, Feng; Ning, Xuyang; Bi, Jingli; Qu, Yang; Liu, Hongfei published an article.Electric Literature of 574-98-1 The title of the article was Hypoxia responsive and tumor-targeted mixed micelles for enhanced cancer therapy and real-time imaging. And the article contained the following:

Most chemotherapy agents have serious side effects due to lack of tumor targeting, which affects their clin. application. In addition, as an essential characteristic of malignant tumor, hypoxia is attracting exclusive research focus regarding its non-invasive real-time tracing in novel targeting delivery system. Herein, we designed a mixed micelle with tumor targeting and hypoxia responsiveness for tumor therapy and imaging. In particular, the dual-modified mix micelles were self-assembled by folic acid (FA) and 2-(2-nitroimidazole) ethylamine (NI) conjugated polymers, in which paclitaxel (PTX) and quantum dots (QDs) were co-loaded into the hydrophobic core. The drug loaded micelles showed satisfactory drug encapsulation, good storage stability, and sustained release properties. In vitro cell experiments showed that the mixed micelles exhibited enhanced cytotoxic effect and improved the cellular uptake, especially under hypoxic conditions, which was due to the FA mediated active targeting effect and NI induced hypoxic responsive release. In vivo experiments further proved that the mixed micelles possessed outstanding tumor targeting and hypoxia responsive properties. Furthermore, the drug loaded micelles showed excellent anti-tumor effect and can realize real-time in vivo imaging. This work demonstrates that the dual-modified mixed micelles co-loading with PTX and QDs might provide a novel approach for tumor therapy and imaging. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Electric Literature of 574-98-1

The Article related to folic acid nitroimidazoleethylamine polymer hypoxia tumor targeted micelle antitumor, hypoxia responsiveness, paclitaxel, quantum dots, real-time imaging, targeted deliver and other aspects.Electric Literature of 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On September 30, 2022, Takao, Go; Hakozaki, Tomohiro; Miura, Keisuke; Urushibara, Yusuke; Fuchibe, Kohei; Ichikawa, Junji published an article.Electric Literature of 2567-29-5 The title of the article was Construction of Substituted [4]Acene Frameworks Based on Double Cationic Cyclizations of Fluoroalkenes. And the article contained the following:

5-Substituted and 5,6-disubstituted [4]acenes were synthesized by the double cationic cyclization of fluoroalkenes. (a) After being treated with Me2AlCl (1.2 equiv), 2-trifluoromethyl-1-alkenes bearing two aryl groups underwent domino Friedel-Crafts-type cyclization (two-ring construction) followed by dehydrogenation to generate 5-fluorinated [4]acenes. The same (trifluoromethyl)alkenes were treated with both Me2AlCl (1.2 equiv) and Me3Al (1.0 equiv), resulting in selective one-ring construction and the creation of bicyclic 1,1-difluoro-1-alkenes. (b) When treated with triflic acid, the bicyclic difluoroalkenes underwent regioselective protonation to generate CF2 cations; Friedel-Crafts-type cyclization of these cations provided tetracyclic ketones. The obtained ketones act as an appropriate platform for the introduction of substituents at the 5-position of [4]acenes. (c) When treated with DDQ/H+, the bicyclic difluoroalkenes underwent oxidative generation of allylic CF2 cations; Friedel-Crafts-type cyclization of these cations produced tetracyclic enones. The enones were subjected to double addition of carbanions to facilitate the introduction of two substituents at the 5- and 6-positions of dihydro[4]acenes. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Electric Literature of 2567-29-5

The Article related to trifluoromethyl alkene regioselective friedel crafts cyclization, polyacene preparation, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Other Tricyclic and Multicyclic Six-Membered Ring Systems, Including Trypticenes and Helicenes and other aspects.Electric Literature of 2567-29-5

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On January 31, 2022, Gao, Yong; Fu, Zhenda; Wu, Di; Yin, Hongquan; Chen, Fu-Xue published an article.Formula: C13H11Br The title of the article was Organocatalyzed Asymmetric Tandem Intramolecular oxa-Michael Addition/Electrophilic Thiocyanation: Synthesis of Chiral α-Thiocyanato Flavanones. And the article contained the following:

An efficient bifunctional cinchona alkaloids-catalyzed asym. tandem intramol. oxa-Michael addition/electrophilic thiocyanation of alkylidene β-ketoesters with N-thiocyanatosuccinimide (NTS) was developed. A series of chiral α-thiocyanato flavanones containing two vicinal stereocenters including an all-carbon quaternary center I [R1 = H, 7-Me, 6-Cl; R2 = Ph, 2-naphthyl, 2-thienyl, etc.; R3 = Me, Et, t-Bu] were prepared in good yields with excellent diastereo- and enantioselectivities (up to 97% ee) under mild conditions, and a successful scale up preparation of our protocol was also demonstrated. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Formula: C13H11Br

The Article related to chiral thiocyanato flavanone preparation, alkylidene ketoester thiocyanatosuccinimide asym tandem michael addition thiocyanation organocatalyst, Heterocyclic Compounds (One Hetero Atom): Benzopyrans (Including Coumarins, Isocoumarins, Chromones, Benzopyrones, Dibenzopyrans, and Other Arenopyrans) and other aspects.Formula: C13H11Br

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On September 3, 2020, He, Chen; Han, Wen-Yong; Cui, Bao-Dong; Wan, Nan-Wei; Chen, Yong-Zheng published an article.Reference of 4-(Bromomethyl)-1,1′-biphenyl The title of the article was Efficient Assembly of Molecular Complexity Enabled by Palladium-Catalyzed Heck Coupling/C(sp2)-H Activation/ C(sp3)-H Activation Cascade. And the article contained the following:

A palladium-catalyzed [2+2+1] annulation among 3-iodochromones, benzyl bromides, and norbornene has been developed. This annulation consists of a domino sequence involving Heck coupling/C(sp2)-H activation/C(sp3)-H activation, affording a variety of complex chromone derivatives I (R = H, 6-Me, 7-F, etc.; R1 = C6H5, 3-MeC6H4, 4-FC6H4, etc.) bearing five contiguous tertiary carbon centers in up to 94% yield and 99:1 dr. Interestingly, the diastereoselectivity could be switched by fine-tuning the solvent, in which endo isomer and exo isomer were obtained using mesitylene/CH3CN and mesitylene, resp. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Reference of 4-(Bromomethyl)-1,1′-biphenyl

The Article related to chromone preparation diastereoselective palladium catalyst, iodochromone benzyl bromide norbornene heck coupling carbon hydrogen activation, Heterocyclic Compounds (One Hetero Atom): Benzopyrans (Including Coumarins, Isocoumarins, Chromones, Benzopyrones, Dibenzopyrans, and Other Arenopyrans) and other aspects.Reference of 4-(Bromomethyl)-1,1′-biphenyl

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On July 31, 2022, Jing, Ke; Wei, Ming-Kai; Yan, Si-Shun; Liao, Li-Li; Niu, Ya-Nan; Luo, Shu-Ping; Yu, Bo; Yu, Da-Gang published an article.Application In Synthesis of 4-(Bromomethyl)-1,1′-biphenyl The title of the article was Visible-light photoredox-catalyzed carboxylation of benzyl halides with CO2: Mild and transition-metal-free. And the article contained the following:

The visible-light photoredox-catalyzed carboxylation of benzyl chlorides and bromides with CO2 has been reported. With inexpensive organic dyes as photocatalysts and amines as electron donors, this carboxylation proceeds well in the absence of sensitive organometallic reagents, transition metal catalysts, or metallic reductants. A wide range of com. available and inexpensive benzyl halides undergo such carboxylation to give valuable aryl acetic acids, including several pharmaceutical mols. and drug precursors, in moderate to high yields. Moreover, this reaction features mild reaction conditions (one atm. pressure of CO2 and room temperature), broad substrate scope, good functional group tolerance, easy scalability, and low catalyst loading, thus providing an efficient approach for the assembly of aryl acetic acids. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Application In Synthesis of 4-(Bromomethyl)-1,1′-biphenyl

The Article related to aryl acetic acid preparation visible light, benzyl chloride bromide carbon dioxide carboxylation photoredox catalyst, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Carboxylic Acids and Peroxycarboxylic Acids and Their Sulfur-Containing Analogs and Salts and other aspects.Application In Synthesis of 4-(Bromomethyl)-1,1′-biphenyl

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On March 31, 2020, Rodriguez-Cruz, Mario A.; Hernandez-Ortega, Simon; Valdes, Hugo; Rufino-Felipe, Ernesto; Morales-Morales, David published an article.Category: bromides-buliding-blocks The title of the article was C-S cross-coupling catalyzed by a series of easily accessible, well defined Ni(II) complexes of the type [(NHC)Ni(Cp)(Br)]. And the article contained the following:

The synthesis, characterization and catalytic evaluation of a series of NHC-Ni(II) complexes I [R = Me, n-Bu, Bn] bearing a phthalimide fragment and a cyclopentadienyl (Cp) ligand was reported. The complexes were evaluated in C-S couplings of iodobenzene and a range of thiols to give thioethers R1-S-R2 [R1 = Ph; R2 = t-Bu, 4-FC6H4, 2-naphthyl, etc.]. The reactions were carried out using a catalyst loading of 5 mol % in DMF during 0.5-19 h. Complex I [R = n-Bu] was the one exhibited the best activity for these transformations yielding up to 96% of products in 0.5 h. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Category: bromides-buliding-blocks

The Article related to nhc based nickel complex preparation, thioether preparation, thiol iodobenzene carbon sulfur cross coupling nickel catalyst, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Phenols, Thiophenols, and Derivatives Including Phenol and Thiophenol Ethers and Esters and other aspects.Category: bromides-buliding-blocks

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On May 20, 2022, Wu, Gaorong; Yang, Zhaoziyuan; Xu, Xiaobo; Hao, Liqiang; Chen, Lu; Wang, Yangyang; Ji, Yafei published an article.Related Products of 2567-29-5 The title of the article was Metal-Free Boron-Mediated ortho-C-H Hydroxylation of N-Benzyl-3,4,5-tribromopyrazoles. And the article contained the following:

A novel route was reported for C-H hydroxylation of benzyl compounds directed by a 3,4,5-tribromopyrazole auxiliary via boronation/oxidation using BBr3 and NaBO3·4H2O. The strategy exhibited outstanding site selectivity and afforded the corresponding phenols in moderate to excellent yields under metal-free conditions. Besides, this protocol was achieved in one pot, which is highly promising as a practical method for use in a multistep organic synthetic process. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Related Products of 2567-29-5

The Article related to benzyl tribromopyrazole preparation boron promoter regioselective hydroxylation, phenol preparation, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Phenols, Thiophenols, and Derivatives Including Phenol and Thiophenol Ethers and Esters and other aspects.Related Products of 2567-29-5

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On January 3, 2013, Geneste, Herve; Ochse, Michael; Drescher, Karla; Behl, Berthold; Laplanche, Loic; Dinges, Juergen; Jakob, Clarissa published a patent.Product Details of 1214362-62-5 The title of the patent was Preparation of isoindole carboxamides, pyrrolopyridine carboxamides, and similar compounds as inhibitors of phosphodiesterase type 10A for treating neurological and psychiatric disorders. And the patent contained the following:

The present invention relates to novel carboxamide compounds of general formula I (wherein X1-X4 are N or (un)substituted CH, with provisos; A is O, S, SO, SO2, substituted N, or (un)substituted CH2; Het is monocyclic hetaryl, fused bicyclic hetaryl, or Ph, all of which may be substituted; and R7-R10 are independently H, halo, C1-4 alkyl, etc.), pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties as inhibitors of phosphodiesterase type 10A and are particularly suitable for treating or controlling medical disorders selected from neurol. disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders. Synthetic procedures for preparing I are exemplified. Example compound II was prepared in a 5-step synthesis that culminated in reaction of 4-methyl-[2,4′]bipyridinyl-3-carboxylic acid Me ester and 2-quinolin-2-ylethylamine. In a PDE10A inhibition assay, II had an IC50 <100 nM. The experimental process involved the reaction of Ethyl 2-bromo-6-fluorobenzoate(cas: 1214362-62-5).Product Details of 1214362-62-5

The Article related to isoindole pyrrolopyridine carboxamide preparation inhibitor pde10a neurol psychiatric disorder, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Product Details of 1214362-62-5

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On November 19, 2020, Allen, Bryce K.; Chamberlain, Brian T.; Dwight, Timothy A.; Huang, Huang; Kulkarni, Meghana M.; Lin, Zhixiong; Marino, Kristen A.; Niu, Deqiang; Shechter, Sharon; Swann, Steven published a patent.COA of Formula: C6H5BrN2O2 The title of the patent was Preparation of benzo[b][1,8]naphthyridine acetic acid derivatives as STING modulators useful in treatment and prevention of STING-associated diseases. And the patent contained the following:

The invention relates to preparation of benzonaphthyridine acetic acids(I) or pharmaceutically acceptable salts or esters thereof capable of binding to and modulating the activity of a stimulator of interferon genes (STING) protein. Compounds I wherein X is O, S, CH=CH, etc.; m is 1-3; Y is CN, OH, NH2, etc.; n is 1-4; Z is halo, CN, OH, etc.; etc., are claimed. The example compound II was prepared via multi-step synthesis using Me 2,6-dichloropyridine-3-carboxylic acid as starting material (procedure given). Compounds I were evaluated for their biol. activity (data given). Compounds I are effective modulators of STING, and can be used for the treatment and prevention of diseases caused by or associated with STING. The experimental process involved the reaction of 2-Amino-6-bromonicotinic acid(cas: 1196157-51-3).COA of Formula: C6H5BrN2O2

The Article related to benzonaphthyridine acetic acid preparation sting modulator disease treatment prophylaxis, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.COA of Formula: C6H5BrN2O2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On August 7, 2018, Orteca, Giulia; Tavanti, Francesco; Bednarikova, Zuzana; Gazova, Zuzana; Rigillo, Giovanna; Imbriano, Carol; Basile, Valentina; Asti, Mattia; Rigamonti, Luca; Saladini, Monica; Ferrari, Erika; Menziani, Maria Cristina published an article.Reference of 2-(2-Bromoethyl)isoindoline-1,3-dione The title of the article was Curcumin derivatives and Aβ-fibrillar aggregates: An interactions’ study for diagnostic/therapeutic purposes in neurodegenerative diseases. And the article contained the following:

Several neurodegenerative diseases, like Alzheimer’s (AD), are characterized by amyloid fibrillar deposition of misfolded proteins, and this feature can be exploited for both diagnosis and therapy design. In this paper, structural modifications of curcumin scaffold were examined in order to improve its bioavailability and stability in physiol. conditions, as well as its ability to interfere with β-amyloid fibrils and aggregates. The acid-base behavior of curcumin derivatives, their pharmacokinetic stability in physiol. conditions, and in vitro ability to interfere with Aβ fibrils at different incubation time were investigated. The mechanisms governing these phenomena have been studied at at. level by means of mol. docking and dynamic simulations. Finally, biol. activity of selected curcuminoids has been investigated in vitro to evaluate their safety and efficiency in oxidative stress protection on hippocampal HT-22 mouse cells. Two aromatic rings, π-conjugated structure and H-donor/acceptor substituents on the aromatic rings showed to be the sine qua nonstructural features to provide interaction and disaggregation activity even at very low incubation time (2 h). Computational simulations proved that upon binding the ligands modify the conformational dynamics and/or interact with the amyloidogenic region of the protofibril facilitating disaggregation. Significantly, in vitro results on hippocampal cells pointed out protection against glutamate toxicity and safety when administered at low concentrations (1 μM). On the overall, in view of its higher stability in physiol. conditions with respect to curcumin, of his rapid binding to fibrillar aggregates and strong depolymerizing activity, phthalimide derivative K2F21 appeared a good candidate for both AD diagnostic and therapeutic purposes. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Reference of 2-(2-Bromoethyl)isoindoline-1,3-dione

The Article related to curcumin neurodegenerative disease antialzheimer alzheimer diagnosis, alzheimer’s disease, amyloid β fibrillar aggregates, curcumin-derivatives, hippocampal ht-22 mouse cells, molecular dynamics simulations and other aspects.Reference of 2-(2-Bromoethyl)isoindoline-1,3-dione

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary