Month: February 2023

Borylation of Unactivated C(sp³)-H Bonds with Bromide as a Traceless Directing Group was written by Zhang, Ge;Li, Meng-Yao;Ye, Wen-Bo;He, Zhi-Tao;Feng, Chen-Guo;Lin, Guo-Qiang. And the article was included in Organic Letters in 2021.Electric Literature of C10H11BrO2 This article mentions the following:

A Pd-catalyzed alkyl C-H borylation of aryl bromides with bromide as a traceless directing group is described, providing a convenient approach to access alkyl boronates bearing a 閻?all-C quaternary stereocenter. The protocol features a broad substrate scope, excellent site selectivity, and good functional group tolerance. In the experiment, the researchers used many compounds, for example, Ethyl (2-bromophenyl)acetate (cas: 2178-24-7Electric Literature of C10H11BrO2).

Ethyl (2-bromophenyl)acetate (cas: 2178-24-7) 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. 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.Electric Literature of C10H11BrO2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Orthosteric-allosteric dual inhibitors of PfHT1 as selective antimalarial agents was written by Huang, Jian;Yuan, Yafei;Zhao, Na;Pu, Debing;Tang, Qingxuan;Zhang, Shuo;Luo, Shuchen;Yang, Xikang;Wang, Nan;Xiao, Yu;Zhang, Tuan;Liu, Zhuoyi;Sakata-Kato, Tomoyo;Jiang, Xin;Kato, Nobutaka;Yan, Nieng;Yin, Hang. And the article was included in Proceedings of the National Academy of Sciences of the United States of America in 2021.Recommanded Product: N-(5-Bromopentyl)phthalimide This article mentions the following:

Artemisinin-resistant malaria parasites have emerged and have been spreading, posing a significant public health challenge. Antimalarial drugs with novel mechanisms of action are therefore urgently needed. In this report, we exploit a ‘selective starvation’ strategy by inhibiting Plasmodium falciparum hexose transporter 1 (PfHT1), the sole hexose transporter in P. falciparum, over human glucose transporter 1 (hGLUT1), providing an alternative approach to fight against multidrug-resistant malaria parasites. The crystal structure of hGLUT3, which shares 80% sequence similarity with hGLUT1, was resolved in complex with C3361, a moderate PfHT1-specific inhibitor, at 2.3-闁?resolution Structural comparison between the present hGLUT3-C3361 and our previously reported PfHT1-C3361 confirmed the unique inhibitor binding-induced pocket in PfHT1. We then designed small mols. to simultaneously block the orthosteric and allosteric pockets of PfHT1. Through extensive structure-activity relationship studies, the TH-PF series was identified to selectively inhibit PfHT1 over hGLUT1 and potent against multiple strains of the blood-stage P. falciparum. Our findings shed light on the next-generation chemotherapeutics with a paradigm-shifting structure-based design strategy to simultaneously target the orthosteric and allosteric sites of a transporter. In the experiment, the researchers used many compounds, for example, N-(5-Bromopentyl)phthalimide (cas: 954-81-4Recommanded Product: N-(5-Bromopentyl)phthalimide).

N-(5-Bromopentyl)phthalimide (cas: 954-81-4) belongs to organobromine compounds. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals. Organobromine compounds have fallen under increased scrutiny for their environmental impact. 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.Recommanded Product: N-(5-Bromopentyl)phthalimide

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Synthesis and evaluation of benzenesulfonic acid derivatives as human neutrophil elastase (hNE) inhibitors was written by Xu, Yanzhao;Qi, Na;Wen, Hui;Zhang, Gang;Wang, Yuchen;Cui, Huaqing. And the article was included in Medicinal Chemistry Research in 2021.Name: 3-Bromobenzene-1-sulfonyl fluoride This article mentions the following:

Herein we report our investigation concerning the development of Human neutrophil elastase (hNE) inhibitors for the treatment of Acute Respiratory Distress Syndrome (ARDS). Various benzenesulfonic acid derived compounds were synthesized and evaluated as competitive inhibitors of hNE. Biol. screening revealed that compound 4f shows moderate inhibitory activity (IC50 = 35.2婵炴挾鎷? against hNE. Compound 4f was also superimposed onto the active center of hNE to understand the binding mode. In the experiment, the researchers used many compounds, for example, 3-Bromobenzene-1-sulfonyl fluoride (cas: 454-65-9Name: 3-Bromobenzene-1-sulfonyl fluoride).

3-Bromobenzene-1-sulfonyl fluoride (cas: 454-65-9) 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.Name: 3-Bromobenzene-1-sulfonyl fluoride

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Palladium-catalyzed C-H alkylation of 2-phenylpyridines with alkyl iodides was written by Wang, Xiaoling;Ji, Xiaoming;Shao, Changdong;Zhang, Yu;Zhang, Yanghui. And the article was included in Organic & Biomolecular Chemistry in 2017.Synthetic Route of C5H11BrO This article mentions the following:

Palladium-catalyzed C-H alkylation reaction of 2-phenylpyridines with alkyl iodides was successfully developed. The palladacycles obtained from 2-phenylpyridines act as the key intermediates in the alkylation reaction. In the experiment, the researchers used many compounds, for example, 1-Bromo-4-methoxybutane (cas: 4457-67-4Synthetic Route of C5H11BrO).

1-Bromo-4-methoxybutane (cas: 4457-67-4) 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). In the pharmaceutical industry organo bromine derivatives are used as sedatives, vasodilators, antiseptic agents, and anticancer agents.Synthetic Route of C5H11BrO

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Synthesis and crystal inclusion properties of 1,3,5-tris(para-substituted aryl)benzenes and double-decker phanes was written by Yamato, Takehiko;Hideshima, Chieko;Nagano, Yoshiaki;Tashiro, Masashi. And the article was included in Journal of Chemical Research, Synopses in 1996.COA of Formula: C24H15Br3 This article mentions the following:

A wide range of inclusion behavior is found for 1,3,5-tris(4-hydroxyphenyl)benzene 3 and 1,3,5-tris(4-alkoxyphenyl)benzenes on recrystallization from various solvents; a double-decker phane derived from 3 also forms a crystalline inclusion complex with toluene, but does not give any observable host-guest interaction in solution In the experiment, the researchers used many compounds, for example, 3,3”-Dibromo-5′-(3-bromophenyl)-1,1′:3′,1”-terphenyl (cas: 96761-85-2COA of Formula: C24H15Br3).

3,3”-Dibromo-5′-(3-bromophenyl)-1,1′:3′,1”-terphenyl (cas: 96761-85-2) 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. 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.COA of Formula: C24H15Br3

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Structure-based design of high-affinity fluorescent probes for the neuropeptide Y Y₁ receptor was written by Mueller, Christoph;Gleixner, Jakob;Tahk, Maris-Johanna;Kopanchuk, Sergei;Laasfeld, Tonis;Weinhart, Michael;Schollmeyer, Dieter;Betschart, Martin U.;Luedeke, Steffen;Koch, Pierre;Rinken, Ago;Keller, Max. And the article was included in Journal of Medicinal Chemistry in 2022.Recommanded Product: 1-Bromopyrrolidine-2,5-dione This article mentions the following:

The recent crystallization of the neuropeptide Y Y₁ receptor (Y₁R) in complex with the argininamide-type Y₁R selective antagonist UR-MK299 (2) opened up a new approach toward structure-based design of nonpeptidic Y₁R ligands. We designed novel fluorescent probes showing excellent Y₁R selectivity and, in contrast to previously described fluorescent Y₁R ligands, considerably higher (~100-fold) binding affinity. This was achieved through the attachment of different fluorescent dyes to the diphenylacetyl moiety in 2 via an amine-functionalized linker. The fluorescent ligands exhibited picomolar Y₁R binding affinities (pK_i values of 9.36-9.95) and proved to be Y₁R antagonists, as validated in a Fura-2 calcium assay. The versatile applicability of the probes as tool compounds was demonstrated by flow cytometry- and fluorescence anisotropy-based Y₁R binding studies (saturation and competition binding and association and dissociation kinetics) as well as by widefield and total internal reflection fluorescence (TIRF) microscopy of live tumor cells, revealing that fluorescence was mainly localized at the plasma membrane. In the experiment, the researchers used many compounds, for example, 1-Bromopyrrolidine-2,5-dione (cas: 128-08-5Recommanded Product: 1-Bromopyrrolidine-2,5-dione).

1-Bromopyrrolidine-2,5-dione (cas: 128-08-5) 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闁艰京鐗梤omine 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.Recommanded Product: 1-Bromopyrrolidine-2,5-dione

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Zirconium-Catalyzed Remote Defunctionalization of Alkenes was written by Matt, Christof;Kern, Christoph;Streuff, Jan. And the article was included in ACS Catalysis in 2020.Synthetic Route of C5H11BrO This article mentions the following:

This work introduces a catalytic zirconium chain-walk reaction that in combination with a 閻?heteroatom elimination step enables the cleavage of remote nonactivated carbon-heteroatom bonds. The result is a controlled defunctionalization reaction, which takes place with excellent site selectivity and can be applied to sym. and unsym. alkene chains with ether, amine, and thioether groups. The approach can be used for remote functional group substitution as well, and a preliminary investigation indicates a dissociative chain-walk mechanism. In the experiment, the researchers used many compounds, for example, 1-Bromo-4-methoxybutane (cas: 4457-67-4Synthetic Route of C5H11BrO).

1-Bromo-4-methoxybutane (cas: 4457-67-4) 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. Commercially available organobromine pharmaceuticals include the vasodilator nicergoline, the sedative brotizolam, the anticancer agent pipobroman, and the antiseptic merbromin. Synthetic Route of C5H11BrO

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Synthesis of benzocarbacephem and benzocarbapemen derivatives by copper-promoted intramolecular aromatic substitution was written by Joyeau, Roger;Yadav, Lal D. S.;Wakselman, Michel. And the article was included in Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry (1972-1999) in 1987.Product Details of 2178-24-7 This article mentions the following:

Copper-mediated cyclization of 4-[2-(o-bromophenyl)ethyl]azetidinones and 4-[o-bromophenyl)methyl]azetidinones gave benzocarbacephem and benzocarbapenem derivatives resp. Halogenation of the diastereoisomeric 2-hydroxybenzocarbacephem-4′-carboxylate (I, R = OH) afforded I (R=Cl) as racemic diastereoisomers or I (R = F) as a single racemic diastereoisomer. The free carboxylic acids of I (R = Cl, F) were inactivators of 閻?lactamases. In the experiment, the researchers used many compounds, for example, Ethyl (2-bromophenyl)acetate (cas: 2178-24-7Product Details of 2178-24-7).

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). 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 2178-24-7

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Ni-Catalyzed reductive arylalkylation of unactivated alkenes was written by Jin, Youxiang;Wang, Chuan. And the article was included in Chemical Science in 2019.SDS of cas: 4457-67-4 This article mentions the following:

In this protocol Ni-catalyzed reductive arylalkylation of unactivated alkenes tethered to aryl bromides with primary alkyl bromides was accomplished, which provided a new path to construct diverse benzene-fused carbo- and heterocyclic cores including indanes, tetrahydroisoquinolines, indolines and isochromanes I [R¹ = Me, Et, i-Pr, cyclohexyl; R² = H, Me, Et; R³ = 5-OMe, 5-F, 4-Cl, etc.; R⁴ = CN, OAc, F, etc.; X = CH₂, NH, NMe, O; m = 0,3,4,5,6; n = 0,1]. Notably, this new method circumvented the pregeneration of organometallics and demonstrated high tolerance to a wide range of functional groups. The preliminary mechanistic investigations suggested a reaction pathway with an intermediate reduction In the experiment, the researchers used many compounds, for example, 1-Bromo-4-methoxybutane (cas: 4457-67-4SDS of cas: 4457-67-4).

1-Bromo-4-methoxybutane (cas: 4457-67-4) belongs to organobromine compounds. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals. Organobromine compounds have fallen under increased scrutiny for their environmental impact. 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: 4457-67-4

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Nickel-Catalyzed Cross-Electrophile C(sp³)-Si Coupling of Unactivated Alkyl Bromides with Vinyl Chlorosilanes was written by Duan, Jicheng;Wang, Yuquan;Qi, Liangliang;Guo, Peng;Pang, Xiaobo;Shu, Xing-Zhong. And the article was included in Organic Letters in 2021.Recommanded Product: 1-Bromo-4-methoxybutane This article mentions the following:

Cross-electrophile C-Si coupling has emerged as a promising tool for the construction of organosilanes, but the potential of this method remains largely unexplored. Herein, we report a C(sp³)-Si coupling of unactivated alkyl bromides with vinyl chlorosilanes. The reaction proceeds under mild conditions, and it offers a new approach to alkylsilanes. Functionalities such as Grignard-sensitive groups (e.g., acid, amide, alc., ketone, and ester), acid-sensitive groups (e.g., ketal and THP protection), alkyl fluoride and chloride, aryl bromide, alkyl tosylate and mesylate, silyl ether, and amine were tolerated. Incorporation of the -Si(vinyl)R₂ moiety into complex mols. and the immobilization of a glass surface by formed organosilanes were demonstrated. In the experiment, the researchers used many compounds, for example, 1-Bromo-4-methoxybutane (cas: 4457-67-4Recommanded Product: 1-Bromo-4-methoxybutane).

1-Bromo-4-methoxybutane (cas: 4457-67-4) 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. 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: 1-Bromo-4-methoxybutane

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary