Tag: 200-300

On May 21, 2021, Weis, Erik; Hayes, Martin A.; Johansson, Magnus J.; Martin-Matute, Belen published an article.Application of 1427433-22-4 The title of the article was Iridium-catalyzed C-H methylation and d3-methylation of benzoic acids with application to late-stage functionalizations. And the article contained the following:

An iridium-catalyzed carboxylate-directed ortho C-H methylation and d3-methylation of benzoic acids was reported. The method used com. available reagents and precatalyst and requires no inert atm. or exclusion of moisture. Substrates bearing electron-rich and electron-poor groups were successfully methylated, including compounds with competing directing/coordinating groups. The method was also applied to the LSF of several marketed drugs, forming analogs with increased metabolic stability compared with the parent drug. The experimental process involved the reaction of 3-Bromo-2-fluoro-6-methyl-benzoic acid(cas: 1427433-22-4).Application of 1427433-22-4

The Article related to benzoic acid potassium methyltrifluoroborate iridium catalyst regioselective methylation, methylbenzoic acid preparation, applied chemistry, chemistry, green chemistry, organic chemistry and other aspects.Application of 1427433-22-4

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On November 17, 2021, Bonnefoy, Clemence; Chefdeville, Emmanuel; Panosian, Armen; Hanquet, Gilles; Leroux, Frederic R.; Toulgoat, Fabien; Billard, Thierry published an article.Synthetic Route of 2567-29-5 The title of the article was Study of a Stable “Trifluoromethoxide Anion Solution” Arising from 2,4-Dinitro-Trifluoromethoxybenzene. And the article contained the following:

Despite recent advances, trifluoromethoxylation remains a challenging reaction. Here we describe an efficient trifluoromethoxylative substitution, using an inexpensive and easy-to-handle reagent. By mixing DMAP with a slight excess of 2,4-dinitro-trifluoromethoxybenzene (DNTFB), a stable solution of trifluoromethoxide anion is obtained and can be used to perform a SN2 reaction without any silver additives. A precise study of the properties and behavior of this unusual stable solution of CF3O- species is also performed. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Synthetic Route of 2567-29-5

The Article related to fluoromethoxylative substitution nitrotrifluoromethoxybenzene, 2,4-dinitro-trifluoromethoxybenzene, fluorine, nucleophilic substitution, trifluoromethoxide anion, trifluoromethoxylation and other aspects.Synthetic Route of 2567-29-5

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On October 14, 2021, Reynolds, Dominic; Leger, Serge; Seiler, Michael W.; Agrawal, Anant A.; Vaillancourt, Frederic; Smith, Peter; Hopper, Allen T.; Prajapati, Sudeep; Soueidan, Olivier published a patent.SDS of cas: 1196157-51-3 The title of the patent was Preparation of quinazolinone, phthalazinone and isoquinolinone compounds for modulating splicing. And the patent contained the following:

The present disclosure features compounds I [A = (un)substituted cycloalkyl, heterocyclyl, aryl, or heteroaryl; Rb = B, (un)substituted alkyl, or heteroalkyl; B = (un)substituted cycloalkyl, heterocyclyl, aryl, or heteroaryl; Y = N, (un)substituted CH, or CH2; R2 = (independently) H or alkyl; R3 = (halo)alkyl, halo, cyano, etc.; each of L1 and L2 = (independently) absent, alkylene, heteroalkylene, O, etc.; m = 0-3; n = 0-2] or pharmaceutically acceptable salts, and related compositions that, inter alia, modulate nucleic acid splicing, e.g., splicing of a pre-mRNA, as well as methods of use thereof. E.g., a multi-steps synthesis of II, starting from 2-methyl-2H-indazole-5-carboxylic acid, was described. Exemplified compounds I were tested for their RNA splicing modulatory activity (data given for representative compounds I). Pharmaceutical composition comprising compound I was disclosed. The experimental process involved the reaction of 2-Amino-6-bromonicotinic acid(cas: 1196157-51-3).SDS of cas: 1196157-51-3

The Article related to quinazolinone phthalazinone isoquinolinone preparation splicing nucleic acid rna modulator, premrna dna rna spliceosome modulator quinazolinone phthalazinone isoquinolinone preparation and other aspects.SDS of cas: 1196157-51-3

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On April 1, 2020, Wang, Guowei; Zhu, Dingcheng; Zhou, Zhuxian; Piao, Ying; Tang, Jianbin; Shen, Youqing published an article.COA of Formula: C13H11Br The title of the article was Glutathione-Specific and Intracellularly Labile Polymeric Nanocarrier for Efficient and Safe Cancer Gene Delivery. And the article contained the following:

Cationic polymers condense nucleic acids into nanosized complexes (polyplexes) that are widely explored for nonviral gene delivery, but their strong electrostatic binding with DNA causes inefficient intracellular gene release and translation and thereby unsatisfactory gene transfection efficiencies. Facilitated intracellular dissociation of polyplexes by making the polymer undergo pos.-to-neg./neutral charge reversal can effectively solve these problems, but they must be sufficiently stable during the delivery. Herein, we report the first glutathione (GSH)-specific intracellular labile polyplexes for cancer-targeted gene delivery. The polymers are made from p-(2,4-dinitrophenyloxybenzyl)-ammonium cationic moieties, whose p-2,4-dinitrophenyl ether is cleaved specifically by GSH, rather than other biol. thiols, triggering the conversion of the ammonium cation into the carboxylate anion and thus the fast intracellular DNA release of the polyplexes. Furthermore, the polyplexes coated with PEG-functionalized lipids are stable in biol. fluids to gain long blood circulation for tumor accumulation. Thus, the efficient tumor accumulation and cell transfection of the polyplexes loaded with the tumor suicide gene tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) give rise to potent antitumor activity similar to that of the first-line chemotherapy drug paclitaxel but with much less adverse effects. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).COA of Formula: C13H11Br

The Article related to tumor antitumor trail gene therapy vector glutathione, cancer gene delivery, charge-reversal polymer, gene release, glutathione-responsive polymer, nonviral vectors, polymeric vector and other aspects.COA of Formula: C13H11Br

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On August 31, 2020, Miura, Kazuki; Onodera, Chihiro; Takagi, Motonari; Koyama, Ryosuke; Hirano, Takako; Nishio, Toshiyuki; Hakamata, Wataru published an article.Recommanded Product: 2567-29-5 The title of the article was Screening, synthesis, and evaluation of novel isoflavone derivatives as inhibitors of human Golgi β-galactosidase. And the article contained the following:

The genes GLB1 and GALC encode GLB1 isoform 1 and galactocerebrosidase, resp., which exhibit β-galactosidase activity in human lysosomes. GLB1 isoform 1 has been reported to play roles in rare lysosomal storage diseases. In this study, we first constructed a cell-based high-throughput screening (HTS) system for Golgi β-galactosidase inhibitors, and then screened inhibitors from two compound libraries using the HTS system, in vitro assay, and cytotoxicity assay. An isoflavone derivative was identified among the final Golgi β-galactosidase inhibitor compound hits. Mol. docking simulations were performed to redesign the isoflavone derivative into a more potent inhibitor, and six designed derivatives were then synthesized. One of the derivatives, ARM07, exhibited potent inhibitory activity against β-galactosidase, with an IC50 value of 14.8 μM and competitive inhibition with Ki value of 13.3 μM. Furthermore, the in vitro and cellular inhibitory activities of ARM07 exceeded those of deoxygalactonojirimycin. ARM07 may contribute to the development of affinity-based chem. probes to identify the protein responsible for the newly discovered Golgi β-galactosidase activity. The therapeutic relevance of ARM07 against lysosomal storage diseases and its effect on senescent cells should be evaluated further. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Recommanded Product: 2567-29-5

The Article related to krabbe disease glb1 galactocerebrosidase mol docking simulation, inhibitor screening, isoflavone, lysosomal storage disease, senescence-associated β-galactosidase, β-galactosidase and other aspects.Recommanded Product: 2567-29-5

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On November 11, 2021, Yan, Si-Shun; Liu, Shi-Han; Chen, Lin; Bo, Zhi-Yu; Jing, Ke; Gao, Tian-Yu; Yu, Bo; Lan, Yu; Luo, Shu-Ping; Yu, Da-Gang published an article.Category: bromides-buliding-blocks The title of the article was Visible-light photoredox-catalyzed selective carboxylation of C(sp3)-F bonds with CO2. And the article contained the following:

A novel selective carboxylation of C(sp3)-F bonds with CO2 via visible-light photoredox catalysis. A variety of mono-, di-, and trifluoroalkylarenes as well as α,α-difluorocarboxylic esters and amides undergo such reactions to give important aryl acetic acids and α-fluorocarboxylic acids, including several drugs and analogs, under mild conditions. Notably, mechanistic studies and DFT calculations demonstrate the dual role of CO2 as an electron carrier and electrophile during this transformation. The fluorinated substrates would undergo single-electron reduction by electron-rich CO2 radical anions, which were generated in situ from CO2 via sequential hydride-transfer reduction and hydrogen-atom-transfer processes. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Category: bromides-buliding-blocks

The Article related to fluoroalkylarene 4czipn photocatalyst carboxylation, aryl acetic acid preparation, fluorocarboxylic ester 3dpafipn photocatalyst carboxylation, fluoro carboxylic acid preparation and other aspects.Category: bromides-buliding-blocks

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On September 2, 2005, Chow, Hak-Fun; Low, Kam-Hung; Wong, King Y. published an article.Safety of 2-Bromo-4-(bromomethyl)-1-methylbenzene The title of the article was An improved method for the regiospecific synthesis of polysubstituted [2.2]paracyclophanes. And the article contained the following:

4,16-Disubstituted, 4,7,12,15-tetrasubstituted, 4,8,12,16-tetrasubstituted and 4,5,7,8,12,13,15,16-octasubstituted [2.2]paracyclophanes can be prepared in significantly improved yields and excellent regiospecificities via the Winberg 1,6-elimination-dimerization reaction from substituted (4-methylbenzyl)trimethylammonium hydroxides. Using 2-chlorophenothiazine instead of phenothiazine as a polymerization inhibitor results in a doubling of product yields. The crystal structures of two of the products are available online. The experimental process involved the reaction of 2-Bromo-4-(bromomethyl)-1-methylbenzene(cas: 259231-26-0).Safety of 2-Bromo-4-(bromomethyl)-1-methylbenzene

The Article related to paracyclophane preparation crystal structure, bromoparacyclophane preparation crystal structure, methylbenzylmethylammonium hydroxide preparation winberg elimination dimerization and other aspects.Safety of 2-Bromo-4-(bromomethyl)-1-methylbenzene

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On May 13, 2004, Bit, Rino Antonio; Giblin, Gerard Martin Paul; Hall, Adrian; Hurst, David Nigel; Kilford, Ian Reginald; Miller, Neil Derek; Scoccitti, Tiziana published a patent.Application In Synthesis of Ethyl 2-bromo-6-fluorobenzoate The title of the patent was Preparation of benzoic acids and related compounds as EP1 receptor antagonists for the treatment of prostaglandin mediated diseases.. And the patent contained the following:

Title compounds I [A = (un)substituted aryl, 5 or 6-membered heterocyclyl ring, bicyclic heterocyclyl; B = Ph, pyridyl; Z = O, S, SO, etc.; R1 = CO2R4, CN, CONR5R6, etc.; R2a, R2b = H, halogen, (un)substituted alkyl, etc.; Rx = (un)substituted alkyl, CQaQb-heterocyclyl, CQaQb-bicyclic heterocyclyl, etc.; R4, R5 = H, (un)substituted alkyl; R6 = H, (un)substituted alkyl, heteroaryl, etc.; R8, R9 = H, Cl, F, etc.; Qa, Qb = H, CH3] and their pharmaceutically acceptable derivatives were prepared For example, the Suzuki coupling of Et 2′-bromobiphenyl-3-carboxylate and 2-benzyloxy-5-chlorophenylboronic acid, e.g., prepared from 3-ethoxycarbonylphenylboronic acid, followed by hydrolysis afforded compound I [A-R1 = 3-carboxyphenyl; Z = O; R2a = H, R2b = 5-Cl; R8, R9 = H] in 39% overall yield. In human prostanoid EP1 receptor binding assays, 90-examples of compounds I exhibited pIC50 values ranging from 6.0->9.0 at the EP1 receptor and pIC50 values of <6.0 at the EP3 receptor. Of note, no toxicol. effects are indicated/expected (sic) when the compounds I are administered at the assay concentration of 3 nM. Compounds I are claimed useful for the treatment of prostaglandin mediated diseases, e.g., inflammation, pain, etc. The experimental process involved the reaction of Ethyl 2-bromo-6-fluorobenzoate(cas: 1214362-62-5).Application In Synthesis of Ethyl 2-bromo-6-fluorobenzoate

The Article related to benzoic acid derivative preparation ep1 receptor antagonist prostaglandin disease, antiinflammatory agent benzoic acid derivative preparation ep1 receptor antagonist, analgesic benzoic acid derivative preparation ep1 receptor antagonist and other aspects.Application In Synthesis of Ethyl 2-bromo-6-fluorobenzoate

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Varano, Flavia; Catarzi, Daniela; Vigiani, Erica; Vincenzi, Fabrizio; Pasquini, Silvia; Varani, Katia; Colotta, Vittoria published an article in 2020, the title of the article was Piperazine- and piperidine-containing thiazolo[5,4-d]pyrimidine derivatives as new potent and selective adenosine A2A receptor inverse agonists.Quality Control of 2-(2-Bromoethyl)isoindoline-1,3-dione And the article contains the following content:

The therapeutic use of A2A adenosine receptor (AR) antagonists for the treatment of neurodegenerative disorders, such as Parkinson and Alzheimer diseases, is a very promising approach. Moreover, the potential therapeutic role of A2A AR antagonists to avoid both immunoescaping of tumor cells and tumor development is well documented. Herein, authors report on the synthesis and biol. evaluation of a new set of piperazine- and piperidine- containing 7-amino-2-(furan-2-yl)thiazolo[5,4-d]pyrimidine derivatives designed as human A2A AR antagonists/inverse agonists. Binding and potency data indicated that a good number of potent and selective hA2A AR inverse agonists were found. Amongst them, the compound I exhibited the highest A2A AR binding affinity (Ki = 8.62 nM) as well as inverse agonist potency (IC50 = 7.42 nM). The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Quality Control of 2-(2-Bromoethyl)isoindoline-1,3-dione

The Article related to piperazinyl piperidinyl thiazolopyrimidine preparation in silico adme prediction, adenosine a2a receptor inverse agonist human, g protein-coupled receptors, adenosine a2a receptor ligands, adenosine receptors, thiazolo[5,4-d]pyrimidines and other aspects.Quality Control of 2-(2-Bromoethyl)isoindoline-1,3-dione

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On May 26, 1987, Haga, Toru; Nagano, Hideyoshi; Okuda, Hiroki; Takase, Masayuki published a patent.Computed Properties of 111010-07-2 The title of the patent was Preparation of 5-bromo-4-chloro-2-fluoroaniline as intermediate for tetrahydrophthalimide herbicides. And the patent contained the following:

The title compound (I), useful as an intermediate for herbicidal tetrahydrophthalimides II (R = H, alkyl, Ph) were prepared by reduction of 1-bromo-2-chloro-4-fluoro-5-nitrobenzene (III). A mixture of 14 g III and 20 g Fe powder in AcOH 20, EtOAc 30, and 5% aqueous AcOH 50 mL was refluxed at 60-80° for 3 h to give 10.4 g I. The experimental process involved the reaction of 5-Bromo-4-chloro-2-fluoroaniline(cas: 111010-07-2).Computed Properties of 111010-07-2

The Article related to aniline trihalo preparation herbicide intermediate, herbicide intermediate bromochlorofluoroaniline preparation, phthalimide tetrahydro herbicide intermediate trihaloaniline, bromochlorofluoroaniline intermediate herbicide preparation and other aspects.Computed Properties of 111010-07-2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary