Tag: 200-300

Discovery of Bispecific Antagonists of Retinol Binding Protein 4 That Stabilize Transthyretin Tetramers: Scaffolding Hopping, Optimization, and Preclinical Pharmacological Evaluation as a Potential Therapy for Two Common Age-Related Comorbidities was written by Cioffi, Christopher L.;Muthuraman, Parthasarathy;Raja, Arun;Varadi, Andras;Racz, Boglarka;Petrukhin, Konstantin. And the article was included in Journal of Medicinal Chemistry in 2020.Application In Synthesis of Methyl 3-bromo-4-fluorobenzoate This article mentions the following:

Accumulation of cytotoxic lipofuscin bisretinoids may contribute to atrophic age-related macular degeneration (AMD) pathogenesis. Retinal bisretinoid synthesis depends on the influx of serum all-trans-retinol delivered via a tertiary retinol binding protein 4 (RBP4)-transthyretin (TTR)-retinol complex. We previously identified selective RBP4 antagonists that dissociate circulating RBP4-TTR-retinol complexes, reduce serum RBP4 levels, and inhibit bisretinoid synthesis in models of enhanced retinal lipofuscinogenesis. However, the release of TTR by selective RBP4 antagonists may be associated with TTR tetramer destabilization and, potentially, TTR amyloid formation. We describe herein the identification of bispecific RBP4 antagonist-TTR tetramer kinetic stabilizers. Standout analog I possesses suitable potency for both targets, significantly lowers mouse plasma RBP4 levels, and prevents TTR aggregation in a gel-based assay. This new class of bispecific compounds may be especially important as a therapy for dry AMD patients who have another common age-related comorbidity, senile systemic amyloidosis, a nongenetic disease associated with wild-type TTR misfolding. In the experiment, the researchers used many compounds, for example, Methyl 3-bromo-4-fluorobenzoate (cas: 82702-31-6Application In Synthesis of Methyl 3-bromo-4-fluorobenzoate).

Methyl 3-bromo-4-fluorobenzoate (cas: 82702-31-6) 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. The principal reactions for organobromides include dehydrobromination, Grignard reactions, reductive coupling, and nucleophilic substitution.Application In Synthesis of Methyl 3-bromo-4-fluorobenzoate

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Total Synthesis of Dictyodendrins A-F by the Gold-Catalyzed Cascade Cyclization of Conjugated Diyne with Pyrrole was written by Matsuoka, Junpei;Inuki, Shinsuke;Matsuda, Yuka;Miyamoto, Yoichi;Otani, Mayumi;Oka, Masahiro;Oishi, Shinya;Ohno, Hiroaki. And the article was included in Chemistry – A European Journal in 2020.COA of Formula: C9H11BrO This article mentions the following:

The total synthesis of dictyodendrins A-F was achieved by using the gold(I)-catalyzed annulation of a conjugated diyne with N-Boc-pyrrole for direct construction of the pyrrolo[2,3-c]carbazole scaffold. Late-stage functionalization of the resulting pyrrolo[2,3-c]carbazole to introduce various substituents provided divergent access to dictyodendrins. Some dictyodendrin analogs exhibited inhibitory activities toward CDK2/CycA2 and GSK3. In the experiment, the researchers used many compounds, for example, 1-(2-Bromoethyl)-4-methoxybenzene (cas: 14425-64-0COA of Formula: C9H11BrO).

1-(2-Bromoethyl)-4-methoxybenzene (cas: 14425-64-0) 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. 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.COA of Formula: C9H11BrO

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Synthesis and in-vitro evaluation of platelet aggregation inhibitory activity of paeonol and its analogs was written by Akamanchi, K. G.;Padmawar, P. A.;Thatte, U. M.;Rege, N. N.;Dahanukar, S. A.. And the article was included in Pharmacy and Pharmacology Communications in 1999.Safety of 3-Bromophenyl acetate This article mentions the following:

Paeonol (1-(2-hydroxy-4-methoxyphenyl)ethanone) and a series of substituted 1-(2-hydroxyphenyl)ethanone derivatives were synthesized and screened as inhibitors of platelet aggregation. The compounds with the greatest anti-platelet potential among the series tested were 1-(2,5-dihydroxyphenyl)ethanone (65.36% inhibition at 300 μM against 5 μM ADP), paeonol (36.31%), 1-(2-hydroxy-5-methoxyphenyl)ethanone (24.47%), 1-(2-hydroxy-5-nitrophenyl) ethanone (30.40%), and 1-(5-chloro-2-hydroxy-4-methylphenyl)ethanone (24.43%). In the experiment, the researchers used many compounds, for example, 3-Bromophenyl acetate (cas: 35065-86-2Safety of 3-Bromophenyl acetate).

3-Bromophenyl acetate (cas: 35065-86-2) belongs to organobromine compounds. Bromine is more electronegative than carbon (2.9 vs 2.5). Consequently, the carbon in a carbon–bromine bond is electrophilic, i.e. alkyl bromides are alkylating agents. 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.Safety of 3-Bromophenyl acetate

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Tuning photodynamic properties of BODIPY dyes, porphyrins’ little sisters was written by Krzemien, Wojciech;Rohlickova, Monika;Machacek, Miloslav;Novakova, Veronika;Piskorz, Jaroslaw;Zimcik, Petr. And the article was included in Molecules in 2021.Related Products of 954-81-4 This article mentions the following:

The photodynamic properties of a series of non-halogenated, dibrominated and diiodinated BODIPYs with a phthalimido or amino end modification on the phenoxypentyl and phenoxyoctyl linker in the meso position were investigated. Halogen substitution substantially increased the singlet oxygen production based on the heavy atom effect. This increase was accompanied by a higher photodynamic activity against skin melanoma cancer cells SK-MEL-28, with the best compound reaching an EC₅₀ = 0.052 ± 0.01μM upon light activation. The dark toxicity (toxicity without light activation) of all studied dyes was not detected up to the solubility limit in cell culture medium (10μM). All studied BODIPY derivatives were predominantly found in adiposomes (lipid droplets) with further lower signals colocalized in either endolysosomal vesicles or the endoplasmic reticulum. A detailed investigation of cell death indicated that the compounds act primarily through the induction of apoptosis. In conclusion, halogenation in the 2,6 position of BODIPY dyes is crucial for the efficient photodynamic activity of these photosensitizers. In the experiment, the researchers used many compounds, for example, N-(5-Bromopentyl)phthalimide (cas: 954-81-4Related Products of 954-81-4).

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). 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.Related Products of 954-81-4

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Efficient and Complementary Methods Offering Access to Synthetically Valuable 1,2-Dibromobenzenes was written by Diemer, Vincent;Leroux, Frederic R.;Colobert, Francoise. And the article was included in European Journal of Organic Chemistry in 2011.Name: 3,4-Dibromoaniline This article mentions the following:

1,2-Dibromobenzenes are highly valuable precursors for various organic transformations, in particular, reactions based on the intermediate formation of benzynes. This report describes short sequences for the synthesis of various derivatives based on regioselective bromination, ortho-metalation, and halogen/metal permutations. 1,2-Dibromo-3-iodobenzene, 1,2-dibromo-4-iodobenzene, and 2,3-dibromo-1,4-diiodobenzene act as intermediates in these syntheses. In the experiment, the researchers used many compounds, for example, 3,4-Dibromoaniline (cas: 615-55-4Name: 3,4-Dibromoaniline).

3,4-Dibromoaniline (cas: 615-55-4) 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. Commercially available organobromine pharmaceuticals include the vasodilator nicergoline, the sedative brotizolam, the anticancer agent pipobroman, and the antiseptic merbromin. Name: 3,4-Dibromoaniline

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Bronsted Acid-Catalyzed : Synthesis of Phenanthrenes via Phosphomolybdic Acid as a Catalyst was written by Chen, Yi;Liu, Di;Wang, Rui;Xu, Li;Tan, Jingyao;Shu, Mao;Tian, Lingfeng;Jin, Yuan;Zhang, Xiaoke;Lin, Zhihua. And the article was included in Journal of Organic Chemistry in 2022.Safety of 2-Bromo-4-(trifluoromethyl)benzaldehyde This article mentions the following:

Herein, disclosed a synthetic protocol for the synthesis of phenanthrenes such as I [R = H, Me; R¹ = H, Me, OMe, etc.; R² = H, F, OMe, etc.; R³ = H, OTIPS; R⁴ = H, F, Cl, etc.] through the CCOM with the inexpensive, nontoxic phosphomolybdic acid as a catalyst. The current annulations could realized carbonyl-olefin, carbonyl-alc., and acetal-alc. in situ CCOM reactions and feature mild reaction conditions, simple manipulation and scalability, making this strategy a promising alternative to the Lewis acid-catalyzed COM reaction. In the experiment, the researchers used many compounds, for example, 2-Bromo-4-(trifluoromethyl)benzaldehyde (cas: 85118-24-7Safety of 2-Bromo-4-(trifluoromethyl)benzaldehyde).

2-Bromo-4-(trifluoromethyl)benzaldehyde (cas: 85118-24-7) belongs to organobromine compounds. Bromine is more electronegative than carbon (2.9 vs 2.5). Consequently, the carbon in a carbon–bromine bond is electrophilic, i.e. alkyl bromides are alkylating agents. 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.Safety of 2-Bromo-4-(trifluoromethyl)benzaldehyde

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

(Indolylalkyl)piperidine carbamates as inhibitors of fatty acid amide hydrolase (FAAH) was written by Dahlhaus, Helmut;Hanekamp, Walburga;Lehr, Matthias. And the article was included in MedChemComm in 2017.Quality Control of N-(5-Bromopentyl)phthalimide This article mentions the following:

A series of Ph 4-[(indol-1-yl)alkyl]piperidine carbamates was synthesized and tested for inhibition of the endocannabinoid degrading enzyme fatty acid amide hydrolase (FAAH) and for metabolic stability in rat liver S9 fractions and porcine blood plasma. Structure-activity relationship studies revealed that variation of the length of the alkyl spacer connecting the indole and the piperidine heterocycle, introduction of substituents into the indole ring, replacement of the piperidine by a piperazine scaffold as well as opening of the piperidine ring system affect activity significantly. The metabolic stability of this compound class proved to be significantly higher than that of corresponding Ph N-(indol-1-ylalkyl)carbamates. In the experiment, the researchers used many compounds, for example, N-(5-Bromopentyl)phthalimide (cas: 954-81-4Quality Control of N-(5-Bromopentyl)phthalimide).

N-(5-Bromopentyl)phthalimide (cas: 954-81-4) belongs to organobromine compounds. Most organobromine compounds, like most organohalide compounds, are relatively nonpolar. 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.Quality Control of N-(5-Bromopentyl)phthalimide

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Localized versus Backbone Fluorescence in N-p-(Diarylboryl)phenyl-Substituted 2,7- and 3,6-Linked Polycarbazoles was written by Reitzenstein, Doerte;Lambert, Christoph. And the article was included in Macromolecules (Washington, DC, United States) in 2009.Related Products of 100189-84-2 This article mentions the following:

The triarylborane acceptor in poly[9-((4-dimesitylboryl)-3,5-dimethylphenyl)-9H-carbazole]-3,6-diyl, P2, has a strong impact on the optical properties of the 3,6-linked polycarbazole and results in enhanced fluorescence quantum yield because of a low-lying fluorescent CT (charge transfer) state. In contrast, the same acceptor substituent does not influence the optical properties of poly[9-((4-dimesitylboryl)-3,5-dimethylphenyl)-9H-carbazole]-2,7-diyl, P1. In P1, the optical properties are governed by conjugation along the carbazole backbone. This interpretation is supported by comparison with poly[9-(4-(diphenylmethyl)-phenyl)-9H-carbazole]-2,7-diyl, P3, reference Synthesis and characterization by gel permeation chromatog., NMR spectroscopy, absorption, and fluorescence measurements in solution and solid state and cyclic voltammetric measurements of the three polymers are presented. A single-layer OLED [organic light-emitting device] was constructed with P2 to study electroluminescent properties. A solution of P2 in chloroform/toluene was spin coated onto ITO-coated glass plates, and Al contacts were deposited on top. In the experiment, the researchers used many compounds, for example, 2,5-Dibromo-1,3-dimethylbenzene (cas: 100189-84-2Related Products of 100189-84-2).

2,5-Dibromo-1,3-dimethylbenzene (cas: 100189-84-2) 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.Related Products of 100189-84-2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Enantioselective Synthesis of 3-Methyleneindan-1-ols via a One-Pot Allylboration-Heck Reaction of 2-Bromobenzaldehydes was written by Calder, Ewen D. D.;Sutherland, Andrew. And the article was included in Organic Letters in 2015.Application In Synthesis of 2-Bromo-4-(trifluoromethyl)benzaldehyde This article mentions the following:

A novel, one-pot allylboration-Heck reaction of 2-bromobenzaldehydes has been developed for the general and efficient synthesis of 3-methyleneindan-1-ols I [R = 6-OMe, 5-Me, 6-F, etc.]. Modification of the one-pot procedure to include chiral Bronsted acid catalyzed allylation has allowed the preparation of these building blocks in high enantioselectivity and excellent yields. In the experiment, the researchers used many compounds, for example, 2-Bromo-4-(trifluoromethyl)benzaldehyde (cas: 85118-24-7Application In Synthesis of 2-Bromo-4-(trifluoromethyl)benzaldehyde).

2-Bromo-4-(trifluoromethyl)benzaldehyde (cas: 85118-24-7) belongs to organobromine compounds. Most organobromine compounds, like most organohalide compounds, are relatively nonpolar. Commercially available organobromine pharmaceuticals include the vasodilator nicergoline, the sedative brotizolam, the anticancer agent pipobroman, and the antiseptic merbromin. Application In Synthesis of 2-Bromo-4-(trifluoromethyl)benzaldehyde

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

A controlled and selective bromination of phenols by benzyltriphenylphosphonium tribromide was written by Hajipour, Abdol Reza;Mallakpour, Shadpour E.;Imanieh, Hassein;Pourmousavi, Seied Ali. And the article was included in Journal of Chemical Research, Synopses in 2002.Category: bromides-buliding-blocks This article mentions the following:

Reactions of phenols with benzyltriphenylphosphonium tribromide in dichloromethane-MeOH mixture (2:1) gave mono, di and tri brominated phenols at room temperature with high selectivity and good yields. In the experiment, the researchers used many compounds, for example, 4-Bromo-2-chloro-6-nitrophenol (cas: 58349-01-2Category: bromides-buliding-blocks).

4-Bromo-2-chloro-6-nitrophenol (cas: 58349-01-2) 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.Category: bromides-buliding-blocks

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary