Tag: 200-300

A Scalable Synthesis of Roxadustat (FG-4592) was written by Pisa, Ondrej;Radl, Stanislav;Cerna, Igor;Sembera, Filip. And the article was included in Organic Process Research & Development in 2022.Safety of Methyl 2-bromo-4-fluorobenzoate This article mentions the following:

A scalable five-step protocol for synthesis of roxadustat, an orally administered hypoxia-inducible factor-Pr hydroxylase inhibitor (HIF-PHI), were developed with an emphasis placed on aspects of medicinal chem. The isoquinoline core of the mol. was prepared using a purposefully designed cyclocondensation in which both the cyclocondensation and demasking of the groups being condensed is promoted by a common acid agent in one step. Roxadustat were obtained pure in a very competitive overall yield across all reaction steps and in compliance with permissible residual Pd level in API. In the experiment, the researchers used many compounds, for example, Methyl 2-bromo-4-fluorobenzoate (cas: 653-92-9Safety of Methyl 2-bromo-4-fluorobenzoate).

Methyl 2-bromo-4-fluorobenzoate (cas: 653-92-9) 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. 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.Safety of Methyl 2-bromo-4-fluorobenzoate

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Palladium-catalyzed 8-exo trig intramolecular Heck reaction under microwave irradiation in the presence of basic alumina was written by Saha, Pritam;Mondal, Shyamal;Hazra, Abhijit;Naskar, Subhendu;Maity, Arindam;Sahu, Krishnendu B.;Paira, Rupankar;Das, Saktipada;Banerjee, Sukdeb;Mondal, Nirup B.. And the article was included in Synthetic Communications in 2012.HPLC of Formula: 61150-57-0 This article mentions the following:

The Heck cross-coupling reaction was employed for efficient conversion of quinolines to benzoxocinoquinoline through a microwave-assisted palladium-catalyzed intramol. cyclization in the presence of basic alumina. In the experiment, the researchers used many compounds, for example, 2-Bromo-4-fluorobenzylbromide (cas: 61150-57-0HPLC of Formula: 61150-57-0).

2-Bromo-4-fluorobenzylbromide (cas: 61150-57-0) 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.HPLC of Formula: 61150-57-0

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Identification of 2-(2′-fluoro-[1,1′-biphenyl]-2-yl)acetamide as a Sodium Valproate-like broad spectrum anti-epileptic drug candidate was written by Tanaka, Tomoyuki;Yajima, Nana;Kiyoshi, Tomoko;Miura, Yoshiki;Inoue, Yoshifumi;Nishimaki, Takuya;Iwama, Seiji. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2019.Related Products of 2178-24-7 This article mentions the following:

By further optimizing compound A [2′-fluoro-N-methyl-[1,1′-biphenyl]-2-sulfonamide], we identified DSP-0565 [2-(2′-fluoro-[1,1′-biphenyl]-2-yl)acetamide, 17a] as a strong, broad-spectrum anti-epileptic drug (AED) candidate. Our efforts mainly focused on finding an alternative polar group for the sulfonamide in order to improve ADME profile of compound A including good metabolic stability and no reactive metabolic production This led to the identification of biphenyl acetamide as a new scaffold for development of broad-spectrum AED candidates. DSP-0565 showed anti-convulsant activity in various models (scPTZ, MES, 6 Hz and amygdala kindling) with good safety margin, and was therefore selected as a clin. candidate. In the experiment, the researchers used many compounds, for example, Ethyl (2-bromophenyl)acetate (cas: 2178-24-7Related Products of 2178-24-7).

Ethyl (2-bromophenyl)acetate (cas: 2178-24-7) 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 2178-24-7

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Identification of anti-HIV agents with a novel benzo[4,5]isothiazolo[2,3-a]pyrimidine scaffold was written by Okazaki, Shiho;Mizuhara, Tsukasa;Shimura, Kazuya;Murayama, Hiroto;Ohno, Hiroaki;Oishi, Shinya;Matsuoka, Masao;Fujii, Nobutaka. And the article was included in Bioorganic & Medicinal Chemistry in 2015.Recommanded Product: 85118-24-7 This article mentions the following:

3,4-Dihydro-2H-benzo[4,5]isothiazolo[2,3-a]pyrimidine is a newly identified antiviral agent against human immunodeficiency virus type 1 (HIV-1) infection, derived from 3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine (PD 404182). The introduction of the hydrophobic 8-aryl substituent on the benzene substructure improved its anti-HIV activity, resulting in the identification of 6-fold more potent analogs. In addition, it was demonstrated that these isothiazolopyrimidine derivatives exert anti-HIV effects at an early stage of viral infection. In the experiment, the researchers used many compounds, for example, 2-Bromo-4-(trifluoromethyl)benzaldehyde (cas: 85118-24-7Recommanded Product: 85118-24-7).

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. 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.Recommanded Product: 85118-24-7

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Discovery of a Novel Series of Biphenyl Benzoic Acid Derivatives as Potent and Selective Human β₃-Adrenergic Receptor Agonists with Good Oral Bioavailability. Part I was written by Imanishi, Masashi;Tomishima, Yasuyo;Itou, Shinji;Hamashima, Hitoshi;Nakajima, Yutaka;Washizuka, Kenichi;Sakurai, Minoru;Matsui, Shigeo;Imamura, Emiko;Ueshima, Koji;Yamamoto, Takao;Yamamoto, Nobuhiro;Ishikawa, Hirofumi;Nakano, Keiko;Unami, Naoko;Hamada, Kaori;Matsumura, Yasuhiro;Takamura, Fujiko;Hattori, Kouji. And the article was included in Journal of Medicinal Chemistry in 2008.SDS of cas: 179232-29-2 This article mentions the following:

A novel class of biphenyl analogs containing a benzoic acid moiety based on lead compound I have been identified as potent and selective human β₃ adrenergic receptor (β₃-AR) agonists with good oral bioavailability and long plasma half-life. After further substituent effects were investigated at the terminal Ph ring of lead compound I, it has been discovered that more lipophilic substitution at the R position improved potency and selectivity. As a result of these studies, II and III were identified as the leading candidates with the best balance of potency, selectivity, and pharmacokinetic profiles. In addition, compounds II and III were evaluated to be efficacious for a carbachol-induced increase of intravesical pressure, such as an overactive bladder model in anesthetized dogs. This represents the first demonstrated result dealing with β₃-AR agonists. In the experiment, the researchers used many compounds, for example, Methyl 4-bromo-2-fluorobenzoate (cas: 179232-29-2SDS of cas: 179232-29-2).

Methyl 4-bromo-2-fluorobenzoate (cas: 179232-29-2) 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). 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: 179232-29-2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Nickel-Catalyzed Oxidative Decarboxylative Annulation for the Synthesis of Heterocycle-Containing Phenanthridinones was written by Honeycutt, Aaron P.;Hoover, Jessica M.. And the article was included in Organic Letters in 2018.Related Products of 29241-66-5 This article mentions the following:

A nickel-catalyzed oxidative decarboxylative annulation reaction of simple benzamides and (hetero)aromatic carboxylates has been developed. This reaction provides access to a large array of phenanthridinones, e.g. I, and their heterocyclic analogs, highlighting the utility and versatility of oxidative decarboxylative coupling strategies for C-C bond formation. In the experiment, the researchers used many compounds, for example, 5-Bromo-2-fluoronicotinic acid (cas: 29241-66-5Related Products of 29241-66-5).

5-Bromo-2-fluoronicotinic acid (cas: 29241-66-5) 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. 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.Related Products of 29241-66-5

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Sterically Shielded Heptamethine Cyanine Dyes for Bioconjugation and High Performance Near-Infrared Fluorescence Imaging was written by Li, Dong-Hao;Schreiber, Cynthia L.;Smith, Bradley D.. And the article was included in Angewandte Chemie, International Edition in 2020.Safety of 2,5-Dibromo-1,3-dimethylbenzene This article mentions the following:

The near-IR window of fluorescent heptamethine cyanine dyes greatly facilitates biol. imaging because there is deep penetration of the light and negligible background fluorescence. However, dye instability, aggregation, and poor pharmacokinetics are current drawbacks that limit performance and the scope of possible applications. All these limitations are simultaneously overcome with a new mol. design strategy that produces a charge balanced and sterically shielded fluorochrome. The key design feature is a meso-aryl group that simultaneously projects two shielding arms directly over each face of a linear heptamethine polyene. Cell and mouse imaging experiments compared a shielded heptamethine cyanine dye (and several peptide and antibody bioconjugates) to benchmark heptamethine dyes and found that the shielded systems possess an unsurpassed combination of photophys., physiochem., and biodistribution properties that greatly enhance bioimaging performance. In the experiment, the researchers used many compounds, for example, 2,5-Dibromo-1,3-dimethylbenzene (cas: 100189-84-2Safety of 2,5-Dibromo-1,3-dimethylbenzene).

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

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Apical Functionalization of Chiral Heterohelicenes was written by Surampudi, Sravan K.;Nagarjuna, G.;Okamoto, Daiki;Chaudhuri, Piyali D.;Venkataraman, D.. And the article was included in Journal of Organic Chemistry in 2012.Product Details of 100189-84-2 This article mentions the following:

We describe a synthetic protocol to selectively functionalize chiral bridged triarylamines at the apical position using regioselective copper-catalyzed amination reaction. This protocol allows the coupling of diphenylamines with a sterically hindered but electronically activated aryl-Br bond in the presence of a sterically unhindered but electronically unactivated aryl-Br bond. The unactivated aryl-Br bond was utilized further to synthesize a chiral heterohelicene homodimer using Stille coupling. In the experiment, the researchers used many compounds, for example, 2,5-Dibromo-1,3-dimethylbenzene (cas: 100189-84-2Product Details of 100189-84-2).

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

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Mn(III)-Mediated Radical Cyclization of o-Alkenyl Aromatic Isocyanides with Boronic Acids: Access to N-Unprotected 2-Aryl-3-cyanoindoles was written by Liu, Lu;Li, Lei;Wang, Xin;Sun, Ran;Zhou, Ming-Dong;Wang, He. And the article was included in Organic Letters in 2021.Name: 1-(Bromomethyl)-4-fluoro-2-nitrobenzene This article mentions the following:

The synthesis of N-unprotected 2-aryl-3-cyanoindoles was realized via the Mn(III)-mediated radical cascade cyclization of o-alkenyl aromatic isocyanides with boronic acids. A possible mechanism involving a sequential intermol. radical addition, intramol. cyclization, and cleavage of the C-C bond under mild reaction conditions is proposed. Mechanism studies show that H₂O or O₂ might provide the oxygen source for the elimination of benzaldehyde. In the experiment, the researchers used many compounds, for example, 1-(Bromomethyl)-4-fluoro-2-nitrobenzene (cas: 76437-44-0Name: 1-(Bromomethyl)-4-fluoro-2-nitrobenzene).

1-(Bromomethyl)-4-fluoro-2-nitrobenzene (cas: 76437-44-0) 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. In the pharmaceutical industry organo bromine derivatives are used as sedatives, vasodilators, antiseptic agents, and anticancer agents.Name: 1-(Bromomethyl)-4-fluoro-2-nitrobenzene

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Ruthenium-catalyzed selective synthesis of monoalkylated barbituric acids through “borrowing hydrogen” methodology was written by Putra, Anggi Eka;Oe, Yohei;Ohta, Tetsuo. And the article was included in Tetrahedron Letters in 2017.COA of Formula: C7H7BrO2 This article mentions the following:

An environmentally benign alkylation of barbituric acids via “borrowing hydrogen” process with ruthenium catalysis was established. The corresponding 5-(alkyl)barubituric acids were obtained in good to excellent yields with low catalyst loading. Various substrates including aliphatic alcs. were tolerated in the present catalytic system. A novel method for construction of barbituric acid-fused benzopyrane derivatives was also demonstrated. In the experiment, the researchers used many compounds, for example, 5-Bromo-2-(hydroxymethyl)phenol (cas: 170434-11-4COA of Formula: C7H7BrO2).

5-Bromo-2-(hydroxymethyl)phenol (cas: 170434-11-4) belongs to organobromine compounds. Most organobromine compounds, like most organohalide compounds, are relatively nonpolar. 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: C7H7BrO2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary