Category: bromides-buliding-blocks

Novel 1-(prop-2-yn-1-ylamino)-2,3-dihydro-1H-indene-4-thiol derivatives as potent selective human monoamine oxidase B inhibitors: Design, SAR development, and biological evaluation was written by Kong, Haiyan;Meng, Xianshe;Hou, Rui;Yang, Xiaoxiao;Han, Jihong;Xie, Zhouling;Duan, Yajun;Liao, Chenzhong. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2021.Application of 14425-64-0 This article mentions the following:

Successes have been achieved in developing human monoamine oxidase B (hMAO-B) inhibitors as anti-Parkinson’s disease (PD) drugs. However, low efficiency and unwanted side effects of the marketed hMAO-B inhibitors hamper their medical applications, therefore, novel potent selective hMAO-B inhibitors are still of great interest. Herein we report 1-(prop-2-yn-1-ylamino)-2,3-dihydro-1H-indene-4-thiol derivatives as hMAO-B inhibitors, which were designed by employing a fragment-based drug design strategy to link rasagiline to hydrophobic fragments. Among the synthesized 31 compounds, I and II demonstrated very encouraging hMAO-B inhibitory activities and selectivity over hMAO-A, better than rasagiline and safinamide. In vitro studies indicated that K8 and K24 are nontoxic to nervous tissue cells and they have considerable effects against ROS formation and potential neuroprotective activity. Further mice behavioral tests demonstrated these two compounds have good therapeutic effects on MPTP-induced PD model mice. All these experiment results suggest that compounds K8 and K24 can be promising candidates for further research for treatment of PD. In the experiment, the researchers used many compounds, for example, 1-(2-Bromoethyl)-4-methoxybenzene (cas: 14425-64-0Application of 14425-64-0).

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. 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.Application of 14425-64-0

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Development of DHQ-based chemical biology probe to profile cellular targets for HBV was written by Zhang, Qing;Huang, Jianzhou;Chow, Hoi Yee;Wang, Jinzheng;Zhang, Yingjun;Fung, Yi Man Eva;Ren, Qingyun;Li, Xuechen. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2020.Safety of Methyl 4-bromo-2-fluorobenzoate This article mentions the following:

Chronic hepatitis B virus (HBV) infection has been a serious public health burden worldwide. Current anti-HBV therapies could not eliminate HBV ultimately. Considering the characteristics of HBV, it is impossible to be entirely cured based on current therapies. Therefore, it is urgently needed to develop novel therapeutic agents with new mechanism of action. The dihydroquinolizinone (DHQ) derivatives exhibited potent anti-HBV activity by decreasing HBV DNA and HBsAg level in an obscure mechanism of action. In this study, we have optimized the DHQ scaffold, developed the photoaffinity probe, with which to identify potential binding proteins. In the experiment, the researchers used many compounds, for example, Methyl 4-bromo-2-fluorobenzoate (cas: 179232-29-2Safety of Methyl 4-bromo-2-fluorobenzoate).

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). 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.Safety of Methyl 4-bromo-2-fluorobenzoate

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Silver complexes [Ph₃PCH₂CH₂PPh₃]²⁺[Ag₂Cl₄]^2-, [Ph₃PCH₂OCH₃]⁺₂[Ag₂Cl₄]^2-, [Ph₃P(i-Am)]⁺₂[Ag₂Br₄]^2-, [Ph₃PC₆H₁₁-cyclo]⁺₂[Ag₂Br₄]^2-, [Ph₃PCH₂Ph]⁺₂[Ag₂Br₄]^2-, and [Ph₃PCH:CH₂]⁺_n[Ag₂Br₃]^–_n, [Me₄P]⁺_n[Ag₂Br₃]^–_n: Synthesis and structure was written by Sharutin, V. V.;Sharutina, O. K.;Senchurin, V. S.;Neudachina, A. N.. And the article was included in Russian Journal of Inorganic Chemistry in 2016.Recommanded Product: Isopentyltriphenylphosphonium bromide This article mentions the following:

Silver complexes [Ph₃PCH₂CH₂PPh₃]²⁺[Ag₂Cl₄]^2- (1), [Ph₃PCH₂OCH₃]⁺₂[Ag₂Cl₄]^2- (2), [Ph₃P(i-Am)]⁺₂[Ag₂Br₄]^2- (3), [Ph₃PC₆H₁₁-cyclo]⁺₂[Ag₂Br₄]^2- (4), [Ph₃PCH₂Ph]⁺₂[Ag₂Br₄]^2- (5), [Ph₃PCH:CH₂]_n⁺[Ag₂Br₃]_n^n- (6), and [Me₄P]_n⁺[Ag₂Br₃]_n^n- (7) have been synthesized by the reaction between tetraorganylphosphonium halides and silver chloride or silver bromide in dimethylsulfoxide. According to x-ray diffraction data, the ionic complexes are built of tetraorganylphosphonium cations and binuclear (1–5) or polynuclear (6, 7) anions. In the anions of complexes 6 and 7, silver atoms are tetracoordinated, and bromine atoms have coordination numbers of 2 and 4. In the experiment, the researchers used many compounds, for example, Isopentyltriphenylphosphonium bromide (cas: 28322-40-9Recommanded Product: Isopentyltriphenylphosphonium bromide).

Isopentyltriphenylphosphonium bromide (cas: 28322-40-9) 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. The principal reactions for organobromides include dehydrobromination, Grignard reactions, reductive coupling, and nucleophilic substitution.Recommanded Product: Isopentyltriphenylphosphonium bromide

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Design, Synthesis, and Structure-Activity Relationship Study of Novel Indole-2-carboxamide Derivatives as Anti-inflammatory Agents for the Treatment of Sepsis was written by Liu, Zhiguo;Tang, Longguang;Zhu, Heping;Xu, Tingting;Qiu, Chenyu;Zheng, Suqing;Gu, Yugui;Feng, Jianpeng;Zhang, Yali;Liang, Guang. And the article was included in Journal of Medicinal Chemistry in 2016.Product Details of 83902-02-7 This article mentions the following:

Sepsis is characterized by a systemic inflammatory response syndrome. Derivatives of indole have been reported to exhibit diverse biol. activities. This study reports on the design and synthesis of a new series of indole-2-carboxamide derivatives, which are screened for their anti-inflammatory activities in RAW 264.7 macrophages. A majority of these derivatives effectively inhibited lipopolysaccharides (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6). Preliminary structure-activity relationship anal. was also conducted. The results indicate that the most promising compounds in the prepared series were 14f and 14g. They were found to effectively reduce LPS-induced pulmonary inflammation and overexpression of a series of inflammatory mediators. Furthermore, in vivo administration of 14f and 14g resulted in remarkable lung histopathol. improvements in mice without toxicity in organs. Taken together, these data indicate that the newly discovered indole-2-carboxamide derivatives could be particularly useful for further treatment in inflammatory diseases. In the experiment, the researchers used many compounds, for example, 2-(Bromomethyl)-1,3-dimethylbenzene (cas: 83902-02-7Product Details of 83902-02-7).

2-(Bromomethyl)-1,3-dimethylbenzene (cas: 83902-02-7) 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. alpha-Bromoesters are employed in the Reformatsky reaction for the synthesis of beta-hydroxyesters. 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.Product Details of 83902-02-7

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Palladium-Catalyzed Enantioselective C(sp²)-H Imidoylation by Desymmetrization was written by Wang, Jian;Gao, De-Wei;Huang, Jinbo;Tang, Shi;Xiong, Zhuang;Hu, Huaanzi;You, Shu-Li;Zhu, Qiang. And the article was included in ACS Catalysis in 2017.Recommanded Product: 61150-57-0 This article mentions the following:

An efficient palladium-catalyzed enantioselective isocyanide insertion/desymmetrizing C(sp²)-H bond activation reaction allowed by a SPINOL-derived phosphoramidite ligand was developed. 3,4-Dihydroisoquinolines containing C3 quaternary stereogenic centers, e.g., I, were obtained in high yields with good enantioselectivity under mild conditions. In the experiment, the researchers used many compounds, for example, 2-Bromo-4-fluorobenzylbromide (cas: 61150-57-0Recommanded Product: 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 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: 61150-57-0

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Synthesis of symmetrical cyclodextrin derivatives bearing multiple charges was written by Guillo, Frederique;Hamelin, Bertrand;Jullien, Ludovic;Canceill, Josette;Lehn, Jean-Marie;De Robertis, Laurence;Driguez, Hugues. And the article was included in Bulletin de la Societe Chimique de France in 1995.Safety of Heptakis(6-Bromo-6-Deoxy)-β-Cyclodextrin This article mentions the following:

Several water-soluble sym. cyclodextrin derivatives bearing pos. charged or neg. charged groups were synthesized to examine the possibility of obtaining stable electrostatically linked hetero-dimers in water. The pos. charged species were obtained from per-amino functionalization of the 6-glucose positions, whereas the neg. units were obtained through introduction of thioglycolate or glycolate groups at the 6- or 3-glucose positions. In the experiment, the researchers used many compounds, for example, Heptakis(6-Bromo-6-Deoxy)-β-Cyclodextrin (cas: 53784-83-1Safety of Heptakis(6-Bromo-6-Deoxy)-β-Cyclodextrin).

Heptakis(6-Bromo-6-Deoxy)-β-Cyclodextrin (cas: 53784-83-1) 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. Commercially available organobromine pharmaceuticals include the vasodilator nicergoline, the sedative brotizolam, the anticancer agent pipobroman, and the antiseptic merbromin. Safety of Heptakis(6-Bromo-6-Deoxy)-β-Cyclodextrin

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Component analysis of 450 °C pyrolyzate from benzene/ethanol extractive of Camellia oleifera cakes was written by Mo, Wei;Zhang, Dang-quan;Li, Bi-xia;Gu, Zhen-jun;Chen, Rong;Ye, Xiao-fei;Peng, Kuan;Zhang, Xiao-lei. And the article was included in Zhongnan Linye Keji Daxue Xuebao in 2015.Synthetic Route of C15H29BrO2 This article mentions the following:

Camellia oleifera cake was firstly lyophilized and extracted by Soxhlet extraction method, the benzene/ethanol extractive was treated with a thermal cracking process in He-flow at 450°C, and then the thermal-cracking product was analyzed by online Py-GC/MS, the relative contents of each component were computed by adopting chromatog. peak area normalization method, a total of 30 compounds were identified. The anal. results show that the pyrolyzate of the benzene/ethanol extractives contains various kinds of precious biomedical, spicery ingredients and specific chems., which are of great potentialities for high-grade cosmetics and skin care products, as well as excellent materials for food, dye and solvent industries. The findings provide new developing directions for deep processing and utilization of Camellia oleifera cakes resources. In the experiment, the researchers used many compounds, for example, 15-Bromopentadecanoic acid (cas: 56523-59-2Synthetic Route of C15H29BrO2).

15-Bromopentadecanoic acid (cas: 56523-59-2) 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.Synthetic Route of C15H29BrO2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Discovery of 4-Benzyloxybenzo[d]isoxazole-3-amine Derivatives as Highly Selective and Orally Efficacious Human Sphingomyelin Synthase 2 Inhibitors that Reduce Chronic Inflammation in db/db Mice was written by Mo, Mingguang;Yang, Jintong;Jiang, Xian-Cheng;Cao, Yu;Fei, Jinyu;Chen, Yang;Qi, Xiangyu;Chu, Yong;Zhou, Lu;Ye, Deyong. And the article was included in Journal of Medicinal Chemistry in 2018.Category: bromides-buliding-blocks This article mentions the following:

Sphingomyelin synthase 2 (SMS2) is a promising therapeutic target for several chronic inflammation-associated diseases, including atherosclerosis, fatty liver and insulin resistance. Herein, we report the identification of 4-benzyloxybenzo[d]isoxazole-3-amine derivatives as potent and highly selective SMS2 inhibitors through a conformational restriction strategy. After systematic structural modifications, several compounds with high selectivity and good potency in vitro were selected for further evaluation. Compound I demonstrated good pharmacokinetics (oral bioavailability, F = 56%) in vivo and has an inhibitory potency against sphingomyelin synthase activity when ICR (Institute of Cancer Research) mice are provided with an oral dose of this compound In addition, compound I attenuated chronic inflammation significantly in db/db mice after oral dosing for 6 wk. In the experiment, the researchers used many compounds, for example, 2-(Bromomethyl)-1,3-dimethylbenzene (cas: 83902-02-7Category: bromides-buliding-blocks).

2-(Bromomethyl)-1,3-dimethylbenzene (cas: 83902-02-7) 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 principal reactions for organobromides include dehydrobromination, Grignard reactions, reductive coupling, and nucleophilic substitution.Category: bromides-buliding-blocks

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Synthesis of new optically active 2-pyrrolidinones was written by Moutevelis-Minakakis, Panagiota;Papavassilopoulou, Eleni;Mavromoustakos, Thomas. And the article was included in Molecules in 2013.Computed Properties of C5H11BrO This article mentions the following:

A new class of optically active 2-pyrrolidinones was synthesized, starting from (S)-pyroglutamic acid, a well known natural chiral synthon. The synthetic design followed led to the insertion of various substituents at positions 1 and 5 of the 2-pyrrolidinone ring, including the imidazole moiety. Some of them possess 2 or 3 stereogenic centers, the configuration of which was retained under the mild conditions used. The new compounds also carry an imidazole moiety, which, along with the 2-pyrrolidinone template, may prove pivotal to several biol. processes. In the experiment, the researchers used many compounds, for example, 1-Bromo-4-methoxybutane (cas: 4457-67-4Computed Properties 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. Computed Properties of C5H11BrO

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

C-H Bond Functionalization in the Synthesis of Fused 1,2,3-Triazoles was written by Panteleev, Jane;Geyer, Karolin;Aguilar-Aguilar, Angelica;Wang, Letian;Lautens, Mark. And the article was included in Organic Letters in 2010.Name: 2-Bromo-4-methyl-6-nitroaniline This article mentions the following:

A highly modular approach to fused 1,2,3-triazoles, e.g. I, has been developed featuring a one-pot procedure combining copper(I) catalyzed azide-alkyne cycloaddition and palladium-catalyzed C-H bond functionalization. A class of structurally unique heterocycles was synthesized in good yields. In the experiment, the researchers used many compounds, for example, 2-Bromo-4-methyl-6-nitroaniline (cas: 827-24-7Name: 2-Bromo-4-methyl-6-nitroaniline).

2-Bromo-4-methyl-6-nitroaniline (cas: 827-24-7) 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. 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.Name: 2-Bromo-4-methyl-6-nitroaniline

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary