Category: bromides-buliding-blocks

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

Yagupol’skii, L. M.; Burmakov, A. I.; Alekseeva, L. A.; Kunshenko, B. V. published an article in 1973, the title of the article was Fluorination of aromatic carboxylic acids by sulfur tetrafluoride. VIII. Fluorination of spatially hindered aromatic carboxylic acids.HPLC of Formula: 41819-13-0 And the article contains the following content:

Fluorination of benzenetricarboxylic acid (I; R = R1 = R2 = CO2H) by SF4 gave 76% fluoride (I; R = R2 = CF3, R1 = COF) which was hydrolyzed to yield 73% acid (I; R = R2 = CF3, R1 = CO2H). The latter was decarboxylated by heat to give 67% (I; R = R2 = CF3, R1 = H). Analogous fluorination of benzenetetracarboxylic acid (II) gave 84% benzodifuran (III; R = Br). Naphthopyran (IV) was obtained in 63% yield from naphthalic acid. Treatment of mellitic acid by SF4 gave 65% III (R = CF3) and 55% benzotrifuran (V) was obtained by fluorination of the corresponding perchlorobenzotrifuran. The experimental process involved the reaction of 3,6-Dibromobenzene-1,2,4,5-tetracarboxylic acid(cas: 41819-13-0).HPLC of Formula: 41819-13-0

The Article related to fluorination acid sulfur tetrafluoride, benzotrifuran perfluoro, benzodifuran perfluoro, 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.HPLC of Formula: 41819-13-0

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On February 26, 2021, Tang, Benzhong; Qin, Anjun; Wang, Bingnan; Hu, Rongrong; Zhao, Zujin; Wang, Zhiming published a patent.Computed Properties of 83152-22-1 The title of the patent was Preparation method of Moxifloxacin derivative, its application for specific dyeing of cell mitochondrion, and as antibacterial agent. And the patent contained the following:

The invention disclosed a kind of Moxifloxacin derivative, its preparation method and application for specific dyeing of cell mitochondrion, and as antibacterial agent. The claimed compound is shown in structure I (R = triphenylphosphonium, pyridinium, quaternary ammonium; X = monovalent anion; n = 1-17 integer). The claimed compound is prepared with Moxifloxacin and organic cationic alkyl bromide (such as (6-bromohexyl)triphenylphosphonium bromide) via substitution. The prepared compound an realize rapid dyeing identification to microorganism, and shows specificity, high efficiency and sensitivity. The Moxifloxacin derivative has excellent antibacterial effect, and can be used for preparation of reagent for specific dyeing of cell mitochondrion, and dyeing of microorganism with neg. charge on surface, preparation of reagent for distinguishing the state of live and dead of microorganism, and preparation of antibacterial agent. The experimental process involved the reaction of (6-Bromohexyl)triphenylphosphonium bromide(cas: 83152-22-1).Computed Properties of 83152-22-1

The Article related to moxifloxacin derivative preparation substitution dyeing agent, 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.Computed Properties of 83152-22-1

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

Grollier, Kevin; Taponard, Alexis; De Zordo-Banliat, Arnaud; Magnier, Emmanuel; Billard, Thierry published an article in 2020, the title of the article was Metal-free nucleophilic trifluoromethylselenolation via an iodide-mediated umpolung reactivity of trifluoromethylselenotoluenesulfonate.Related Products of 2567-29-5 And the article contains the following content:

Herein, a practical method to generate CF3Se- (and RFSe-) anions from shelf-stable reagents under iodide activation was reported. Metal-free nucleophilic trifluoromethylselenolations have been then performed with this in situ-generated anion. Perfluoroalkylselenolations have also been described. The umpolung reactivity of trifluoromethylselenotoluenesulfonates 4-CH3C6H4S(O)2SeR (R = trifluoromethyl, 1,1,2,2,2-pentafluoroethyl, 1,1,2,2,3,3,4,4,5,5,6,6,6-tridecafluorohexyl) can be performed under reductive or oxidative conditions with alkyl halides R1X (R1 = dodecyl, Bn, (5-nitrofuran-2-yl)methyl, etc.; X = Br, Cl) to give desired products R1SeR. 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 selenide preparation, trifluoromethyl selenotoluenesulfonate alkyl halide perfluoroalkylselenolation, fluorine, nucleophilic substitution, perfluoroalkylselenolation, selenium, trifluoromethylselenolation and other aspects.Related Products of 2567-29-5

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Shu, Chenglin; Liu, Caiping; Wu, Mingyan; Chen, Cheng; Hong, Maochun published an article in 2021, the title of the article was Simultaneous fluorescence and phosphorescence in Zn(II)-zwitterionic coordination polymers with tunable colors.SDS of cas: 2567-29-5 And the article contains the following content:

Three similar ionic-type ligands which can provide ligand-centered charge transfer (LCCT) have been employed to synthesize three isostructural complexes, resp. Due to the coordination of the ligands to the metal centers, all of the above mentioned complexes feature fluorescence and phosphorescence properties simultaneously. The mechanism of the luminous process is ligand-centered charge transfer (LCCT) combined with metal-to-ligand charge transfer (MLCT) processes. More interestingly, one compound manifests tunable colors from yellow to blue emissions involving white emission by varying the temperature and/or excitation wavelength directly. Exptl. and computational results indicate that the differences in luminous properties originate from the ligand distortion combined with different electron states. Thus, this study provides a facile method to synthesize new single-component tunable-color luminescent coordination polymers with simultaneous fluorescence and phosphorescence. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).SDS of cas: 2567-29-5

The Article related to bipyridylmethyl azidobipyridylmethyl carboxylatobipyridylmethyl pyridyldicarboxylate zinc coordination polymer preparation structure, fluorescence phosphorescence zinc zwitterionic polymer tunable color and other aspects.SDS of cas: 2567-29-5

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On May 1, 2020, Varano, Flavia; Catarzi, Daniela; Vincenzi, Fabrizio; Pasquini, Silvia; Pelletier, Julie; Lopes Rangel Fietto, Juliana; Espindola Gelsleichter, Nicolly; Sarlandie, Marine; Guilbaud, Audrey; Sevigny, Jean; Varani, Katia; Colotta, Vittoria published an article.Recommanded Product: 574-98-1 The title of the article was Structural investigation on thiazolo[5,4-d]pyrimidines to obtain dual-acting blockers of CD73 and adenosine A2A receptor as potential antitumor agents. And the article contained the following:

Adenosine pathway, including its generating enzyme (CD73) and its receptors represents a key target for cancer immunotherapy. Here we aimed to search for novel compounds able to co-target the CD73 and the A2A adenosine receptor (A2A AR) as dual-blockers of adenosine generation and activity. The design project was to combine in the same mol. the thiazolo[5,4-d]pyrimidine core, an essential pharmacophoric feature to block the A2A AR, with a benzenesulfonamide group which is a characteristic group of CD73 inhibitors. Most of the reported compounds resulted in inverse agonists of the human (h) A2A AR endowed with high affinity, selectivity and potency. However they were weak inhibitors of CD73 enzyme. Nevertheless, this study can be considered as a starting point to develop more active compounds The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Recommanded Product: 574-98-1

The Article related to cancer immunotherapy a2aar inverse agonists cd37 inhibitor antitumor agents, adenosine a(2a) receptor inverse agonists, antitumor agents, cd73 inhibitors, cancer immunotherapy, thiazolo[5,4-d]pyrimidine and other aspects.Recommanded Product: 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Kwon, Ye-Mi; Kim, Sou Hyun; Jung, Young-Suk; Kwak, Jae-Hwan published an article in 2021, the title of the article was Synthesis and Biological Evaluation of (S)-2-(Substituted arylmethyl)-1-oxo-1,2,3,4-tetrahydropyrazino[1,2-a]indole-3-carboxamide Analogs and Their Synergistic Effect against PTEN-Deficient MDA-MB-468 Cells.Reference of 4-(Bromomethyl)-1,1′-biphenyl And the article contains the following content:

A series of twenty-six compounds of furfuryl or benzyl tetrahydropyrazino[1,2-a]indole analogs were synthesized and evaluated for cytotoxic activity against the estrogen receptor (ER)-pos. breast cancer cell line (MCF-7) and the epidermal growth factor receptor (EGFR) over-expressed triple-neg. breast cancer cell line (MDA-MB-468). Among them, compounds 2b, 2f and 2i showed more potent activity and selectivity against MDA-MB-468 cells than gefitinib, as an EGFR- tyrosine kinase inhibitor. In addition, it was confirmed by means of isobologram anal. of combinational treatment with gefitinib that they have a synergistic effect, especially compounds 2b and 2f, which inhibit Akt T308 phosphorylation. Moreover, it was confirmed that 2-benzyl-1-oxo-1,2,3,4-tetrahydropyrazino[1,2-a]indole-3-carboxamide analogs (2b, 2f, and Ref 2) tend to selectively inhibit PI3Kβ, which is involved in the phosphorylation of Akt. 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 arylmethyl tetrahydropyrazinoindole carboxamide analog synergistic effect pten cancer cell, egfr-tki resistance, pten-deficient cancer cells, anti-tnbc, pyrazinoindolone scaffold, synergistic effects and other aspects.Reference of 4-(Bromomethyl)-1,1′-biphenyl

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Sisto, Francesca; Carradori, Simone; Guglielmi, Paolo; Spano, Mattia; Secci, Daniela; Granese, Arianna; Sobolev, Anatoly P.; Grande, Rossella; Campestre, Cristina; Marcantonio, Maria Carmela Di; Mincione, Gabriella published an article in 2021, the title of the article was Synthesis and evaluation of thymol-based synthetic derivatives as dual-action inhibitors against different strains of H. pylori and AGS cell line.Related Products of 2567-29-5 And the article contains the following content:

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. 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 thymol ether preparation helicobacter pylori antibacterial gastric adenocarcinoma, ags cells, helicobacter pylori, drug resistance, dual-action agents, antimicrobial activity, semi-synthesis, thymol and other aspects.Related Products of 2567-29-5

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary