Tag: 200-300

Structure-Based Optimization of Benzoic Acids as Inhibitors of Protein Tyrosine Phosphatase 1B and Low Molecular Weight Protein Tyrosine Phosphatase was written by Maccari, Rosanna;Ottana, Rosaria;Ciurleo, Rosella;Paoli, Paolo;Manao, Giampaolo;Camici, Guido;Laggner, Christian;Langer, Thierry. And the article was included in ChemMedChem in 2009.Formula: C8H7BrO2 This article mentions the following:

Protein Tyrosine Phosphatases comprise a large family of over 100 enzymes. Defective or inappropriate functioning of PTPs has been associated with many human pathologies, including diabetes,obesity and cancer.This communication concentrates on the focus of increasing interest of PTP’s as novel mol. targets in drug design. In the experiment, the researchers used many compounds, for example, 3-(Bromomethyl)benzoic acid (cas: 6515-58-8Formula: C8H7BrO2).

3-(Bromomethyl)benzoic acid (cas: 6515-58-8) belongs to organobromine compounds. Most of the natural organobromine compounds are produced by marine organisms, and several brominated metabolites with antibacterial, antitumor, antiviral, and antifungal activity have been isolated from seaweed, sponges, corals, molluscs, and others. Bromine-containing agents predominate because not only are they more efficient than similar chlorine-containing species, but also the high atomic weight of bromine ensures that it is present in a high mass fraction within most organobromine compounds.Formula: C8H7BrO2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Rh(III)-Catalyzed Phosphine Oxide Migration Reactions: Selective Synthesis of 3-Phosphinoylindoles was written by Wang, Chun-Hai;Yang, Shang-Dong. And the article was included in Chemistry – An Asian Journal in 2018.Formula: C8H4BrF3O This article mentions the following:

3-Phosphinoylindoles are important components of biol. active natural products and materials in pharmaceuticals. Herein, a new approach for the synthesis of 3-phosphinoylindoles was established by a Rh(III)-catalyzed cyclization from readily accessible (2-azidostyryl)diphenylphosphine oxides. This intramol. transformation occurs through a unique phosphine oxide group migration and offers a straightforward route to rebuild sp² C-P bond and construct the indole ring in single step. In the experiment, the researchers used many compounds, for example, 2-Bromo-4-(trifluoromethyl)benzaldehyde (cas: 85118-24-7Formula: C8H4BrF3O).

2-Bromo-4-(trifluoromethyl)benzaldehyde (cas: 85118-24-7) belongs to organobromine compounds. Many of the organo bromine compounds are relatively nonpolar. Bromine is more electronegative than carbon (2.8 vs 2.5) and hence the carbon in a carbon–bromine bond is electrophilic in nature. In the pharmaceutical industry organo bromine derivatives are used as sedatives, vasodilators, antiseptic agents, and anticancer agents.Formula: C8H4BrF3O

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

The First Fluorescent Diboronic Acid Sensor Specific for Hepatocellular Carcinoma Cells Expressing Sialyl Lewis X was written by Yang, Wenqian;Fan, Haiying;Gao, Xingming;Gao, Shouhai;Karnati, Vishnu Vardhan Reddy;Ni, Weijuan;Hooks, W. Borden;Carson, John;Weston, Brent;Wang, Binghe. And the article was included in Chemistry & Biology in 2004.Recommanded Product: 166821-88-1 This article mentions the following:

Carbohydrate antigens with subterminal fucosylation have been implicated in the development and progression of several cancers, including hepatocellular carcinoma (HCC). Fluorescent sensors targeting fucosylated carbohydrate antigens could potentially be used for diagnostic and other applications. The authors have designed and synthesized a series of 26 diboronic acid compounds as potential fluorescent sensors for such carbohydrates. Among these compounds, 7q was able to fluorescently label cells expressing high levels of sLex (HEPG2) within a concentration range of 0.5 to 10 μM. This compound (7q) did not label cells expressing Lewis Y (HEP3B), nor cells without fucosylated antigens (COS7). This represents the first example of a fluorescent compound labeling cells based on cell surface carbohydrate structures. In the experiment, the researchers used many compounds, for example, 2-(2-(Bromomethyl)phenyl)-5,5-dimethyl-1,3,2-dioxaborinane (cas: 166821-88-1Recommanded Product: 166821-88-1).

2-(2-(Bromomethyl)phenyl)-5,5-dimethyl-1,3,2-dioxaborinane (cas: 166821-88-1) belongs to organobromine compounds. Bromo compounds are employed in a variety of metal-catalyzed coupling reactions. They are also ideal candidates for the synthesis of Grignard reagents that have wide-applicability in organic synthesis. alpha-Bromoesters are employed in the Reformatsky reaction for the synthesis of beta-hydroxyesters. Many of the alkyl bromine derivatives are excellent alkylating agents since bromides are good leaving groups. Tribromides, like tetrabutylammonium tribromide, are used as a solid source of bromine. N-bromosuccimide (NBS) is used for the selective bromination of allylic bonds.Recommanded Product: 166821-88-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Mononuclear Copper(II)-Superoxo Complexes that Mimic the Structure and Reactivity of the Active Centers of PHM and DβM was written by Kunishita, Atsushi;Kubo, Minoru;Sugimoto, Hideki;Ogura, Takashi;Sato, Kazunobu;Takui, Takeji;Itoh, Shinobu. And the article was included in Journal of the American Chemical Society in 2009.HPLC of Formula: 14425-64-0 This article mentions the following:

Mononuclear Cu(II)-superoxo complexes 2^X-OO^{â€?/sup> (I) having triplet (S = 1) ground states were obtained via reaction of O₂ with the Cu(I) starting materials 1X (II) supported by tridentate ligands LX [1-(2-p-X-phenethyl)-5-(2-pyridin-2-ylethyl)-1,5-diazacyclooctane; X = CH₃, H, NO₂] in various solvents. The superoxo complexes 2X-OOâ€?/sup> (I) mimic the structure [tetrahedral geometry with an end-on (η1)-bound O₂â€?] and the aliphatic C-H bond activation chem. of peptidylglycine α-hydroxylating monooxygenase and dopamine β-monooxygenase. In the experiment, the researchers used many compounds, for example, 1-(2-Bromoethyl)-4-methoxybenzene (cas: 14425-64-0HPLC of Formula: 14425-64-0).}

1-(2-Bromoethyl)-4-methoxybenzene (cas: 14425-64-0) belongs to organobromine compounds. Many of the organo bromine compounds are relatively nonpolar. Bromine is more electronegative than carbon (2.8 vs 2.5) and hence the carbon in a carbon–bromine bond is electrophilic in nature. One prominent application of synthetic organobromine compounds is the use of polybrominated diphenyl ethers as fire-retardants, and in fact fire-retardant manufacture is currently the major industrial use of the element bromine.HPLC of Formula: 14425-64-0

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

In situ Catalytic Generation of Allylcopper Species for Asymmetric Allylation: Toward 1H-Isochromene Skeletons was written by Kawai, Junya;Chikkade, Prasanna Kumara;Shimizu, Yohei;Kanai, Motomu. And the article was included in Angewandte Chemie, International Edition in 2013.Recommanded Product: 653-92-9 This article mentions the following:

Allylcopper species can be generated in situ via catalytic intramol. oxycupration of allenic alc. The allylcopper can react with various aldehydes and a ketone to give 1H-isochromene derivatives enantioselectively. The protocol is atom-economical, highly regioselective, stereoconvergent, and tolerant to free OH groups. Thus, e.g., enantio- and regioselective oxycupration/asym. addition cascade reaction of allenic alc. I with benzaldehyde in presence of mesitylcopper and chiral diphosphine ligand in HMPA/THF afforded isochromene II (98% yield, 92% ee). In the experiment, the researchers used many compounds, for example, Methyl 2-bromo-4-fluorobenzoate (cas: 653-92-9Recommanded Product: 653-92-9).

Methyl 2-bromo-4-fluorobenzoate (cas: 653-92-9) belongs to organobromine compounds. Many of the organo bromine compounds are relatively nonpolar. Bromine is more electronegative than carbon (2.8 vs 2.5) and hence the carbon in a carbon–bromine bond is electrophilic in nature. When the molecular ion is detected, the bromine and chlorine isotope patterns are very distinct, but caution is to be exercised for certain mixed chlorinated/brominated compounds, which can look similar to homohalogen patterns.Recommanded Product: 653-92-9

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Identification of Transthyretin Tetramer Kinetic Stabilizers That Are Capable of Inhibiting the Retinol-Dependent Retinol Binding Protein 4-Transthyretin Interaction: Potential Novel Therapeutics for Macular Degeneration, Transthyretin Amyloidosis, and Their Common Age-Related Comorbidities was written by Cioffi, Christopher L.;Raja, Arun;Muthuraman, Parthasarathy;Jayaraman, Aravindan;Jayakumar, Srinivasan;Varadi, Andras;Racz, Boglarka;Petrukhin, Konstantin. And the article was included in Journal of Medicinal Chemistry in 2021.HPLC of Formula: 82702-31-6 This article mentions the following:

Dissociation of transthyretin (TTR) tetramers may lead to misfolding and aggregation of proamyloidogenic monomers, which underlies TTR amyloidosis (ATTR) pathophysiol. ATTR is a progressive disease resulting from the deposition of toxic fibrils in tissues that predominantly presents clin. as amyloid cardiomyopathy and peripheral polyneuropathy. Ligands that bind to and kinetically stabilize TTR tetramers prohibit their dissociation and may prevent ATTR onset. Drawing from clin. investigated AG10, we designed a constrained congener (14) that exhibits excellent TTR tetramer binding potency, prevents TTR aggregation in a gel-based assay, and possesses desirable pharmacokinetics in mice. Addnl., 14 significantly lowers murine serum retinol binding protein 4 (RBP4) levels despite a lack of binding at that protein′s all-trans-retinol site. We hypothesize that kinetic stabilization of TTR tetramers via14 is allosterically hindering all-trans-retinol-dependent RBP4-TTR tertiary complex formation and that the compound could present ancillary therapeutic utility for indications treated with RBP4 antagonists, such as macular degeneration. In the experiment, the researchers used many compounds, for example, Methyl 3-bromo-4-fluorobenzoate (cas: 82702-31-6HPLC of Formula: 82702-31-6).

Methyl 3-bromo-4-fluorobenzoate (cas: 82702-31-6) belongs to organobromine compounds. Organo bromine compounds are versatile compounds and are widely used in diverse fields. Organo bromine derivatives are used in the dye sector, as an indicator in analytical chemistry (Bromothymol blue is a popular indicator). The reactivity of organobromine compounds resembles but is intermediate between the reactivity of organochlorine and organoiodine compounds. For many applications, organobromides represent a compromise of reactivity and cost.HPLC of Formula: 82702-31-6

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

8-Aminoquinolines as anticoccidials – part III was written by Armer, Richard E.;Barlow, Jacqueline S.;Chopra, Narinder;Dutton, Christopher J.;Greenway, David H. J.;Greenwood, Sean D. W.;Lad, Nita;Shaw, Jonothan;Thompson, Adrian P.;Thong, Kam-Wah;Tommasini, Ivan. And the article was included in Bioorganic & Medicinal Chemistry Letters in 1999.Application In Synthesis of N-(5-Bromopentyl)phthalimide This article mentions the following:

Analogs of the antimalarial pentaquine I in which the nature of the side-chain on the 8-amino position was varied, were prepared and evaluated for anticoccidial activity both in vitro and in vivo. Specifically, both the inter-nitrogen distance and the nature of the terminal amino group were investigated. Novel analogs of equal or improved efficacy in vitro and in vivo to pentaquine were discovered. In the experiment, the researchers used many compounds, for example, N-(5-Bromopentyl)phthalimide (cas: 954-81-4Application In Synthesis of N-(5-Bromopentyl)phthalimide).

N-(5-Bromopentyl)phthalimide (cas: 954-81-4) belongs to organobromine compounds. Organo bromine compounds are versatile compounds and are widely used in diverse fields. Organo bromine derivatives are used in the dye sector, as an indicator in analytical chemistry (Bromothymol blue is a popular indicator). The reactivity of organobromine compounds resembles but is intermediate between the reactivity of organochlorine and organoiodine compounds. For many applications, organobromides represent a compromise of reactivity and cost.Application In Synthesis of N-(5-Bromopentyl)phthalimide

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

A Detailed Study of Irradiation Requirements Towards an Efficient Photochemical Wohl-Ziegler Procedure in Flow was written by Bonfield, Holly E.;Williams, Jason D.;Ooi, Wei Xiang;Leach, Stuart G.;Kerr, William J.;Edwards, Lee J.. And the article was included in ChemPhotoChem in 2018.SDS of cas: 76437-44-0 This article mentions the following:

A platform has been developed to enable standardization of light sources, allowing consistent scale-up from high-throughput screening in batch to flow, using the same pseudo-monochromatic light source. The impact of wavelength and light intensity on a photochem. reaction was evaluated within this platform using the Wohl-Ziegler benzylic bromination of 4-methyl-3-(trifluoromethyl)benzonitrile with N-bromosuccinimide as a model system. It was found that only 40% of the maximum light intensity was required while still maintaining reaction rate, allowing more reliable temperature control and lower energy consumption. The optimized reaction conditions were subsequently applied to a range of synthetically relevant (hetero)aromatic compounds under continuous conditions, exploring the scope of the process within a mild and scalable procedure. In the experiment, the researchers used many compounds, for example, 1-(Bromomethyl)-4-fluoro-2-nitrobenzene (cas: 76437-44-0SDS of cas: 76437-44-0).

1-(Bromomethyl)-4-fluoro-2-nitrobenzene (cas: 76437-44-0) belongs to organobromine compounds. Many of the organo bromine compounds are relatively nonpolar. Bromine is more electronegative than carbon (2.8 vs 2.5) and hence the carbon in a carbon–bromine bond is electrophilic in nature. One prominent application of synthetic organobromine compounds is the use of polybrominated diphenyl ethers as fire-retardants, and in fact fire-retardant manufacture is currently the major industrial use of the element bromine.SDS of cas: 76437-44-0

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Solid-phase synthesis of phenols and pyridinones via arylboronation/oxidation protocol using aryl bromides was written by Lee, Younghee;Kelly, Martha J.. And the article was included in Tetrahedron Letters in 2006.Name: Methyl 3-bromo-5-hydroxybenzoate This article mentions the following:

A sequence of two known reactions, palladium-catalyzed arylboronation of aryl bromide and subsequent oxidation of arylboronate with oxone, has been carried out to prepare functionalized phenols and pyridin-2(1H)-one which were later loaded on to resin for solid-phase synthesis. Using these resin-bound templates, a number of solid-phase methods were developed to generate libraries of substituted phenols and pyridin-2(1H)-one. In the experiment, the researchers used many compounds, for example, Methyl 3-bromo-5-hydroxybenzoate (cas: 192810-12-1Name: Methyl 3-bromo-5-hydroxybenzoate).

Methyl 3-bromo-5-hydroxybenzoate (cas: 192810-12-1) belongs to organobromine compounds. Bromo compounds are employed in a variety of metal-catalyzed coupling reactions. They are also ideal candidates for the synthesis of Grignard reagents that have wide-applicability in organic synthesis. alpha-Bromoesters are employed in the Reformatsky reaction for the synthesis of beta-hydroxyesters. One prominent application of synthetic organobromine compounds is the use of polybrominated diphenyl ethers as fire-retardants, and in fact fire-retardant manufacture is currently the major industrial use of the element bromine.Name: Methyl 3-bromo-5-hydroxybenzoate

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Discovery of Novel 5-(Piperazine-1-carbonyl)pyridin-2(1H)-one Derivatives as Orally eIF4A3-Selective Inhibitors was written by Mizojiri, Ryo;Nakata, Daisuke;Satoh, Yoshihiko;Morishita, Daisuke;Shibata, Sachio;Iwatani-Yoshihara, Misa;Kosugi, Yohei;Kosaka, Mai;Takeda, Junpei;Sasaki, Shigekazu;Takami, Kazuaki;Fukuda, Koichiro;Kamaura, Masahiro;Sasaki, Shinobu;Arai, Ryosuke;Cary, Douglas R.;Imaeda, Yasuhiro. And the article was included in ACS Medicinal Chemistry Letters in 2017.Application In Synthesis of 5-Bromo-6-methoxynicotinic acid This article mentions the following:

Starting from our previous eIF4A3-selective inhibitor I, a novel series of (piperazine-1-carbonyl)pyridin-2(1H)-one derivatives was designed, synthesized, and evaluated for identification of orally bioavailable probe mols. Compounds II and III showed improved physicochem. and ADMET profiles, while maintaining potent and subtype-selective eIF4A3 inhibitory potency. In accord with their promising PK profiles and results from initial in vivo PD studies, compounds II and III showed antitumor efficacy with T/C values of 54% and 29%, resp., without severe body weight loss. Thus, our novel series of compounds represents promising probe mols. for the in vivo pharmacol. study of selective eIF4A3 inhibition. In the experiment, the researchers used many compounds, for example, 5-Bromo-6-methoxynicotinic acid (cas: 1186194-46-6Application In Synthesis of 5-Bromo-6-methoxynicotinic acid).

5-Bromo-6-methoxynicotinic acid (cas: 1186194-46-6) belongs to organobromine compounds. Most organobromine compounds, like most organohalide compounds, are relatively nonpolar. The reactivity of organobromine compounds resembles but is intermediate between the reactivity of organochlorine and organoiodine compounds. For many applications, organobromides represent a compromise of reactivity and cost.Application In Synthesis of 5-Bromo-6-methoxynicotinic acid

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary