Month: February 2023

Identification of a novel fluoropyrrole derivative as a potassium-competitive acid blocker with long duration of action was written by Nishida, Haruyuki;Arikawa, Yasuyoshi;Hirase, Keizo;Imaeda, Toshihiro;Inatomi, Nobuhiro;Hori, Yasunobu;Matsukawa, Jun;Fujioka, Yasushi;Hamada, Teruki;Iida, Motoo;Nishitani, Mitsuyoshi;Imanishi, Akio;Fukui, Hideo;Itoh, Fumio;Kajino, Masahiro. And the article was included in Bioorganic & Medicinal Chemistry in 2017.Recommanded Product: 881676-32-0 This article mentions the following:

With the aim to find a novel long-lasting potassium-competitive acid blocker (P-CAB) that would perfectly overcome the limitations of proton pump inhibitors (PPIs), we tried various approaches based on pyrrole derivative I as a lead compound As part of a comprehensive approach to identification of a new drug, we explored excellent compounds that have low lipophilicity by introducing a polar hetero-aromatic group at position 5 of the pyrrole ring. Among the compounds synthesized, fluoropyrrole derivativeII, which has a 2-fluoro-3-pyridyl group at the fifth position, lower pK_a, and much lower C log P and log D values than I does, showed potent gastric-acid suppressive action resulting from gastric H⁺,K⁺-ATPase inhibition in animal models. Its maximum intragastric pH elevation effect was strong in rats, and its duration of action was much longer than that of either lansoprazole or lead compound I in dogs. Therefore, compound II can be considered a promising new P-CAB with long duration of action. In the experiment, the researchers used many compounds, for example, 5-Bromo-1H-pyrrole-3-carbaldehyde (cas: 881676-32-0Recommanded Product: 881676-32-0).

5-Bromo-1H-pyrrole-3-carbaldehyde (cas: 881676-32-0) belongs to organobromine compounds. Most organobromine compounds, like most organohalide compounds, are relatively nonpolar. 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: 881676-32-0

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Facile NBS/DMSO mediated dibromination of olefins including selected natural products and glycals was written by Ul Lah, Hafiz;Mir, Shabir Ahmad;Hussain, Gulzar;Wani, Rafiq Ahmad;Yousuf, Syed Khalid. And the article was included in Journal of Chemical Sciences (Berlin, Germany) in 2022.Name: 1-Bromopyrrolidine-2,5-dione This article mentions the following:

A highly chemo- and diastereoselective vic-dibromination of olefins was developed. The process employed a readily available N-Bromosuccinimide (NBS)/DMSO reagent system as a bromine source. High substrate scope, simple reaction conditions, application to natural products and glycals makes the process very attractive. In the experiment, the researchers used many compounds, for example, 1-Bromopyrrolidine-2,5-dione (cas: 128-08-5Name: 1-Bromopyrrolidine-2,5-dione).

1-Bromopyrrolidine-2,5-dione (cas: 128-08-5) 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. 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: 1-Bromopyrrolidine-2,5-dione

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Studies of Substituents Impact on the Photophysical Properties of 8-Hydroxyquinoline Derivatives was written by Gao, Li-Bin;Kang, Wu-Kui;Yan, Shi-Hai;Yang, Chun-Peng. And the article was included in Heteroatom Chemistry in 2016.SDS of cas: 18791-79-2 This article mentions the following:

Five new 8-hydroxyquinoline derivatives L1-L5 were synthesized and characterized by different techniques, such as NMR, electrospray ionization mass spectra, elemental anal., UV-visible, and photoluminescence spectra. The structure of (E)-2-{2-[5-(phenylethynyl) thiophen-2-yl]ethenyl}quinolin-8-ol (L3) was confirmed by x-ray crystallog. In this structure, intermol. hydrogen bonds were found between OH hydrogen donors of one monomer and the oxygen atom of the next one. Photophys. studies show that different substitutes affect the absorption wavelength and emission color. In the experiment, the researchers used many compounds, for example, 5-Bromothiophene-3-carbaldehyde (cas: 18791-79-2SDS of cas: 18791-79-2).

5-Bromothiophene-3-carbaldehyde (cas: 18791-79-2) belongs to organobromine compounds. Bromine is more electronegative than carbon (2.9 vs 2.5). Consequently, the carbon in a carbon闂佺偨鍎茶ぐ绲﹐mine bond is electrophilic, i.e. alkyl bromides are alkylating agents. Commercially available organobromine pharmaceuticals include the vasodilator nicergoline, the sedative brotizolam, the anticancer agent pipobroman, and the antiseptic merbromin. SDS of cas: 18791-79-2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

A carbon-13 NMR investigation of [5]metacyclophanes was written by Jenneskens, L. W.;De Kanter, F. J. J.;De Wolf, W. H.;Bickelhaupt, F.. And the article was included in Magnetic Resonance in Chemistry in 1986.COA of Formula: C8H8Br2 This article mentions the following:

¹³C NMR data of [5]metacyclophane, its 8,11-dihalosubstituted derivatives and of some model compounds are reported and discussed. A remarkable downfield shift is observed for the aromatic carbon between the bridging carbons; this is tentatively ascribed to long-range effects of the bridge and to the bending of the aromatic ring. In the experiment, the researchers used many compounds, for example, 2,5-Dibromo-1,3-dimethylbenzene (cas: 100189-84-2COA of Formula: C8H8Br2).

2,5-Dibromo-1,3-dimethylbenzene (cas: 100189-84-2) 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). 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.COA of Formula: C8H8Br2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Antagonists of the human adenosine A_2A receptor. Part 3: Design and synthesis of pyrazolo[3,4-d]pyrimidines, pyrrolo[2,3-d]pyrimidines and 6-arylpurines was written by Gillespie, Roger J.;Cliffe, Ian A.;Dawson, Claire E.;Dourish, Colin T.;Gaur, Suneel;Jordan, Allan M.;Knight, Antony R.;Lerpiniere, Joanne;Misra, Anil;Pratt, Robert M.;Roffey, Jonathan;Stratton, Gemma C.;Upton, Rebecca;Weiss, Scott M.;Williamson, Douglas S.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2008.Recommanded Product: 3-(Bromomethyl)benzoic acid This article mentions the following:

A series of pyrazolo[3,4-d]pyrimidine, pyrrolo[2,3-d]pyrimidine and 6-arylpurine adenosine A_2A antagonists is described. Many examples were highly selective against the human A₁ receptor sub-type and were active in an in vivo model of Parkinson’s disease. In the experiment, the researchers used many compounds, for example, 3-(Bromomethyl)benzoic acid (cas: 6515-58-8Recommanded Product: 3-(Bromomethyl)benzoic acid).

3-(Bromomethyl)benzoic acid (cas: 6515-58-8) 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.Recommanded Product: 3-(Bromomethyl)benzoic acid

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Lewis base-promoted carbon-carbon sp³-sp³ coupling reactions of 濞?silyl silylethers was written by Brekan, Jonathan A.;Chernyak, Dmitri;White, Kolby L.;Scheidt, Karl A.. And the article was included in Chemical Science in 2012.Application In Synthesis of 1-(3-Bromopropyl)-4-methoxybenzene This article mentions the following:

A Lewis base-promoted addition of 濞?silyl silylethers to primary halides has been developed. This new carbon-carbon sp³-sp³ bond-forming process accesses an unconventional reactivity pattern (d¹ synthon) from easily accessible precursors. The strategy accommodates a variety of primary alkyl, allylic and benzylic electrophiles and 濞?silyl silylethers. These d¹ synthons have also been used in the synthesis of cross pinacol and benzil products. Mechanistic studies indicate significant intermol. silyl group exchange during the reaction. In the experiment, the researchers used many compounds, for example, 1-(3-Bromopropyl)-4-methoxybenzene (cas: 57293-19-3Application In Synthesis of 1-(3-Bromopropyl)-4-methoxybenzene).

1-(3-Bromopropyl)-4-methoxybenzene (cas: 57293-19-3) 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. Commercially available organobromine pharmaceuticals include the vasodilator nicergoline, the sedative brotizolam, the anticancer agent pipobroman, and the antiseptic merbromin. Application In Synthesis of 1-(3-Bromopropyl)-4-methoxybenzene

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Expedient synthesis of gem-dialkylbenzyl heterocycles through olefinic hydroarylation was written by Lian, Yajing;Burford, Kristen;Londregan, Allyn T.. And the article was included in Tetrahedron in 2015.Computed Properties of C3H4BrN3 This article mentions the following:

A robust approach to gem-dialkylbenzyl heterocycles has been developed through a triflic acid-catalyzed hydroarylation of olefinic heterocycles. A broad range of substrates containing pyridine, quinoline, pyrazole, triazole and imidazole moieties are shown to be highly compatible with this method. This rapid construction of gem-dialkyl groups should be useful in the synthesis of drug-like mols. containing heterocyclic diversity and in the study of the gem-dialkyl effect. In the experiment, the researchers used many compounds, for example, 4-Bromo-1-methyl-1H-1,2,3-triazole (cas: 13273-53-5Computed Properties of C3H4BrN3).

4-Bromo-1-methyl-1H-1,2,3-triazole (cas: 13273-53-5) belongs to organobromine compounds. Bromine is more electronegative than carbon (2.9 vs 2.5). Consequently, the carbon in a carbon闂佺偨鍎茶ぐ绲﹐mine 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.Computed Properties of C3H4BrN3

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

An iron(II)-based metalloradical system for intramolecular amination of C(sp²)-H and C(sp³)-H bonds: synthetic applications and mechanistic studies was written by Das, Sandip Kumar;Das, Subrata;Ghosh, Supratim;Roy, Satyajit;Pareek, Monika;Roy, Brindaban;Sunoj, Raghavan B.;Chattopadhyay, Buddhadeb. And the article was included in Chemical Science in 2022.Recommanded Product: Ethyl (2-bromophenyl)acetate This article mentions the following:

A catalytic system for intramol. C(sp²)-H and C(sp³)-H amination of substituted tetrazolopyridines was successfully developed. The amination reactions were developed using an iron-porphyrin based catalytic system. It was demonstrated that the same iron-porphyrin based catalytic system efficiently activates both the C(sp²)-H and C(sp³)-H bonds of the tetrazole as well as azide-featuring substrates with a high level of regioselectivity. The method exhibited an excellent functional group tolerance. The method afforded three different classes of high-value N-heterocyclic scaffolds. A number of important late-stage C-H aminations were performed to access important classes of mols. Detailed studies (exptl. and computational) showed that both the C(sp²)-H and C(sp³)-H amination reactions involve a metalloradical activation mechanism, which is different from the previously reported electro-cyclization mechanism. Collectively, this study reports the discovery of a new class of metalloradical activation modes using a base metal catalyst that should find wide application in the context of medicinal chem., drug discovery and industrial applications. In the experiment, the researchers used many compounds, for example, Ethyl (2-bromophenyl)acetate (cas: 2178-24-7Recommanded Product: Ethyl (2-bromophenyl)acetate).

Ethyl (2-bromophenyl)acetate (cas: 2178-24-7) 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 principal reactions for organobromides include dehydrobromination, Grignard reactions, reductive coupling, and nucleophilic substitution.Recommanded Product: Ethyl (2-bromophenyl)acetate

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Semi-quantitative models for identifying potent and selective transthyretin amyloidogenesis inhibitors was written by Connelly, Stephen;Mortenson, David E.;Choi, Sungwook;Wilson, Ian A.;Powers, Evan T.;Kelly, Jeffery W.;Johnson, Steven M.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2017.SDS of cas: 108940-96-1 This article mentions the following:

Rate-limiting dissociation of the tetrameric protein transthyretin (TTR), followed by monomer misfolding and misassembly, appears to cause degenerative diseases in humans known as the transthyretin amyloidoses, based on human genetic, biochem. and pharmacol. evidence. Small mols. that bind to the generally unoccupied thyroxine binding pockets in the native TTR tetramer kinetically stabilize the tetramer, slowing subunit dissociation proportional to the extent that the mols. stabilize the native state over the dissociative transition state-thereby inhibiting amyloidogenesis. Herein, the authors use previously reported structure-activity relationship data to develop two semi-quant. algorithms for identifying the structures of potent and selective transthyretin kinetic stabilizers/amyloidogenesis inhibitors. The viability of these prediction algorithms, in particular the more robust in silico docking model, is perhaps best validated by the clin. success of tafamidis, the first-in-class drug approved in Europe, Japan, South America, and elsewhere for treating transthyretin aggregation-associated familial amyloid polyneuropathy. Tafamidis is also being evaluated in a fully-enrolled placebo-controlled clin. trial for its efficacy against TTR cardiomyopathy. These prediction algorithms will be useful for identifying second generation TTR kinetic stabilizers, should these be needed to ameliorate the central nervous system or ophthalmol. pathol. caused by TTR aggregation in organs not accessed by oral tafamidis administration. In the experiment, the researchers used many compounds, for example, 3,5-Dibromo-4-methoxybenzaldehyde (cas: 108940-96-1SDS of cas: 108940-96-1).

3,5-Dibromo-4-methoxybenzaldehyde (cas: 108940-96-1) 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.SDS of cas: 108940-96-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Features of molecular bromination of aromatic amines was written by Salahov, M. S.;Bagmanov, B. T.;Mustafayeva, F. A.. And the article was included in Azerbaidzhanskii Khimicheskii Zhurnal in 2014.Recommanded Product: 74440-80-5 This article mentions the following:

The peculiarities of mol. bromination of o-, m-, p-substituted anilines in organic media (CHCl₃, CCl₄) and phys.-chem. characteristics of the prepared substances (mono-, di-, tri-, and tetrabromoanilines) reflecting their composition and structure are presented. In the experiment, the researchers used many compounds, for example, 4-Amino-3-bromophenol (cas: 74440-80-5Recommanded Product: 74440-80-5).

4-Amino-3-bromophenol (cas: 74440-80-5) belongs to organobromine compounds. Bromine is more electronegative than carbon (2.9 vs 2.5). Consequently, the carbon in a carbon闂佺偨鍎茶ぐ绲﹐mine bond is electrophilic, i.e. alkyl bromides are alkylating agents. 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: 74440-80-5

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary