Month: February 2023

Divergent Synthesis of Indolenine and Indoline Ring Systems by Palladium-Catalyzed Asymmetric Dearomatization of Indoles was written by Gao, Dong;Jiao, Lei. And the article was included in Angewandte Chemie, International Edition in 2022.Recommanded Product: 85118-24-7 This article mentions the following:

A Pd-catalyzed intermol. asym. spiroannulation of 2,3-disubstituted indoles with internal alkynes was developed for the efficient construction of indoline structures with a C2-quaternary stereocenter. Stereospecific aza-semipinacol rearrangement of these indoline derivatives under acidic conditions afforded indolenine products bearing a C3-quaternary stereocenter, where the migrating group could be controlled by the reaction sequence. The asym. spiroannulation together with the subsequent aza-semipinacol rearrangement enabled a divergent access to dearomatized indole derivatives with either a C3- or a C2-quaternary stereocenter. 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. 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. 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: 85118-24-7

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Discovery of Orally Available Runt-Related Transcription Factor 3 (RUNX3) Modulators for Anticancer Chemotherapy by Epigenetic Activation and Protein Stabilization was written by Yang, Jee Sun;Lee, Chulho;Cho, Misun;Kim, Hyuntae;Kim, Jae Hyun;Choi, Seonghwi;Oh, Soo Jin;Kang, Jong Soon;Jeong, Jin-Hyun;Kim, Hyun-Jung;Han, Gyoonhee. And the article was included in Journal of Medicinal Chemistry in 2015.Category: bromides-buliding-blocks This article mentions the following:

Recently, the authors identified a novel strategy for anticancer chemotherapy by restoring runt-related transcription factor 3 (RUNX3) levels via lactam-based histone deacetylase (HDAC) inhibitors that stabilize RUNX3. Described here are the synthesis, biol. evaluation, and pharmacokinetic evaluation of new synthetic small mols. based on pyridone-based HDAC inhibitors that specifically stabilize RUNX3 by acetylation and regulate its function. Many of the newly synthesized compounds showed favorable RUNX activities, HDAC inhibitory activities, and inhibitory activities on the growth of human cancer cell lines. Notably, one of these new derivatives, I , significantly restored RUNX3 in a dose-dependent manner and showed high metabolic stability, a good pharmacokinetic profile with high oral bioavailability and long half-life, and strong antitumor activity. This study suggests that pyridone-based analogs modulate RUNX3 activity through epigenetic regulation as well as strong transcriptional and post-translational regulation of RUNX3 and could be potential clin. candidates as orally available RUNX3 modulators for the treatment of cancer. In the experiment, the researchers used many compounds, for example, 1-(3-Bromopropyl)-4-methoxybenzene (cas: 57293-19-3Category: bromides-buliding-blocks).

1-(3-Bromopropyl)-4-methoxybenzene (cas: 57293-19-3) 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.Category: bromides-buliding-blocks

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Fluorination of orthothioesters through oxidative desulfurization-fluorination was written by Furuta, Satoru;Kuroboshi, Manabu;Hiyama, Tamejiro. And the article was included in Bulletin of the Chemical Society of Japan in 1998.Reference of 57293-19-3 This article mentions the following:

The oxidative desulfurization-fluorination of orthothioesters of type RCH₂C(SMe)₃ using n-Bu₄NH₂F₃ and 1,3-dibromo-5,5-dimethylhydantoin gave bromodifluorination products RCHBrCF₂SMe in good yields. The products were converted into bromodifluoro olefins RCBr:CF₂ via oxidation and thermolysis. In a similar way, the orthothioesters of type RCH(OH)C(SMe)₃ or RCH(OAc)C(SMe)₃ were fluorinated to afford difluoro ketones RCOCF₂SMe or difluoro acetates RCH(OAc)CF₂SMe, resp. The difluoro acetates were reduced to RCH(OAc)CF₂H by radical reduction The mechanisms are discussed for difluorination accompanied by bromination or oxidation In the experiment, the researchers used many compounds, for example, 1-(3-Bromopropyl)-4-methoxybenzene (cas: 57293-19-3Reference of 57293-19-3).

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. 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.Reference of 57293-19-3

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Deciphering a novel chloramphenicols resistance mechanism: Oxidative inactivation of the propanediol pharmacophore was written by Zhang, Jiayu;Yang, Chao;Hu, Jiahui;Zhang, Yiting;Lai, Yuezheng;Gong, Hongri;Guo, Fangliang;Li, Xiaoyan;Ye, Lin;Li, Bing. And the article was included in Water Research in 2022.Category: bromides-buliding-blocks This article mentions the following:

Expanding knowledge about new types of antibiotic resistance genes is of great significance in dealing with the global antibiotic resistance crisis. Herein, a novel oxidoreductase capO was discovered to be responsible for oxidative inactivation of chloramphenicol and thiamphenicol. The antibiotic resistance mechanism was comprehensively deciphered using multi-omics and multiscale computational approaches. A 66,383 bp DNA fragment carrying capO was shared among four chloramphenicol-resistant strains, and the co-occurrence of capO with a mobile genetic element cluster revealed its potential mobility among different taxa. Metagenomic anal. of 772 datasets indicated that chloramphenicol was the crucial driving factor for the development and accumulation of capO in activated sludge bioreactors treating antibiotic production wastewater. Therefore, we should pay sufficient attention to its possible prevalence and transfer to pathogens, especially in some hotspot environments contaminated with high concentrations of chloramphenicols. This finding significantly expands our knowledge boundary about chloramphenicols resistance mechanisms. In the experiment, the researchers used many compounds, for example, 1-Bromopyrrolidine-2,5-dione (cas: 128-08-5Category: bromides-buliding-blocks).

1-Bromopyrrolidine-2,5-dione (cas: 128-08-5) 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. Category: bromides-buliding-blocks

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Design and Synthesis of Benzenesulfonamide Derivatives as Potent Anti-Influenza Hemagglutinin Inhibitors was written by Tang, Guozhi;Lin, Xianfeng;Qiu, Zongxing;Li, Wentao;Zhu, Lei;Wang, Lisha;Li, Shaohua;Li, Haodong;Lin, Wenbin;Yang, Mei;Guo, Tao;Chen, Li;Lee, Daniel;Wu, Jim Z.;Yang, Wengang. And the article was included in ACS Medicinal Chemistry Letters in 2011.Name: 3-Bromo-5-chlorophenylamine This article mentions the following:

Structural optimization of salicylamide-based hemagglutinin (HA) inhibitor 1 resulted in the identification of cis-3-(5-hydroxy-1,3,3-trimethylcyclohexylmethylamino)benzenesulfonamide 28 and its derivatives as potent anti-influenza agents. The lead compound 28 and its 2-chloro analog 40 can effectively prevent cytopathic effects (CPE) caused by infection of influenza A/Weiss/43 strain (H1N1) with EC₅₀ values of 210 and 86 nM, resp. Mechanism of action studies indicate that 40 and its analogs inhibit the virus fusion with host endosome membrane by binding to HA and stabilizing the prefusion HA structure. With significantly improved metabolic stability, the reported series represents the first generation of orally bioavailable HA inhibitors that have a good selectivity window and potential for further development as novel anti-influenza agents. In the experiment, the researchers used many compounds, for example, 3-Bromo-5-chlorophenylamine (cas: 96558-78-0Name: 3-Bromo-5-chlorophenylamine).

3-Bromo-5-chlorophenylamine (cas: 96558-78-0) 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.Name: 3-Bromo-5-chlorophenylamine

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Non-steroidal aromatase inhibitors based on a biphenyl scaffold: synthesis, in vitro SAR, and molecular modelling was written by Jackson, Toby;Woo, L. W. Lawrence;Trusselle, Melanie N.;Purohit, Atul;Reed, Michael J.;Potter, Barry V. L.. And the article was included in ChemMedChem in 2008.Electric Literature of C7H6BrF This article mentions the following:

The synthesis and in vitro biol. evaluation (JEG-3 cells) of a series of novel and potent aromatase inhibitors, prepared by microwave-enhanced Suzuki cross-coupling methodol., are reported. These compounds possess a biphenyl template incorporated with the haem-ligating triazolylmethyl moiety, either on its own or in combination with other substituent(s) at various positions on the Ph rings. The most potent aromatase inhibitor reported herein has an IC₅₀ value of 0.12 nM, although seven of its congeners are also highly potent (IC₅₀ 闂?0.5 nM). They all bear the (5-triazolylmethyl-2-cyano)biphenyl structural motif. Docking of representative compounds into a homol. model of human aromatase assists in the rationalisation of the SAR derived from the in vitro biol. results and supports a crucial role for a cyano group on the “A” Ph ring, which is accessible to hydrogen bond interactions with Ser478. Further development of these compounds as potential therapeutic agents for the treatment of hormone-dependent breast cancer is warranted given the high level of potency observed for this class of aromatase inhibitor in vitro. In the experiment, the researchers used many compounds, for example, 3-Bromo-4-fluorotoluene (cas: 452-62-0Electric Literature of C7H6BrF).

3-Bromo-4-fluorotoluene (cas: 452-62-0) 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.Electric Literature of C7H6BrF

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Synthesis of novel fluorophenyl, furan tagged benzylthiopyrimidine derivatives was written by Maddila, Suresh;Lavanya, Palakondu;Jonnalagadda, Sreekanth B.. And the article was included in Chemija in 2013.Application of 76437-44-0 This article mentions the following:

A series of 6-(4-fluorophenyl)-2-(substituted benzylthio)-4-(furan-2-yl)-1,6- dihydropyrimidine derivatives I (R = H, 3-F, 4-CH₃, 4-NO₂, etc.) have been synthesized from 2-acetylfuran through a multi-step reaction sequence. The key intermediate II reacted with various substituted benzyl bromides in the presence of K₂CO₃ to afford the desired products, which were characterized by IR, ¹H NMR, LCMS, and elemental anal. In the experiment, the researchers used many compounds, for example, 1-(Bromomethyl)-4-fluoro-2-nitrobenzene (cas: 76437-44-0Application of 76437-44-0).

1-(Bromomethyl)-4-fluoro-2-nitrobenzene (cas: 76437-44-0) 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). 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.Application of 76437-44-0

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Design, synthesis and insecticidal activity of novel anthranilic diamides with benzyl sulfide scaffold was written by Chen, Yin-Bo;Li, Ji-Ling;Shao, Xu-Sheng;Xu, Xiao-Yong;Li, Zhong. And the article was included in Chinese Chemical Letters in 2013.Computed Properties of C8H4BrF3O3 This article mentions the following:

A series of novel anthranilic diamides with benzyl sulfide scaffold were synthesized, in which the N-pyridylpyrazole moiety generally regarded as key pharmacophore was abandoned. Preliminary bioassays indicated that half of the title compounds were endowed with good insecticidal activities against armyworm (Mythimna separata) at 500 mg/L. Exhilaratingly, one of the synthesized compounds was also active against Tetranychus cinnabarinus at 100 mg/L. The difference in activities between the target compounds was influenced by the substituents, which provided some hints for further investigation on structure modifications. In the experiment, the researchers used many compounds, for example, 3-Bromo-5-(trifluoromethoxy)benzoic acid (cas: 453565-90-7Computed Properties of C8H4BrF3O3).

3-Bromo-5-(trifluoromethoxy)benzoic acid (cas: 453565-90-7) 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.Computed Properties of C8H4BrF3O3

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Enantioselective Oxidation of Alkenes with Potassium Permanganate Catalyzed by Chiral Dicationic Bisguanidinium was written by Wang, Chao;Zong, Lili;Tan, Choon-Hong. And the article was included in Journal of the American Chemical Society in 2015.HPLC of Formula: 28322-40-9 This article mentions the following:

Chiral anion-controlled ion-pairing catalysis was demonstrated to be a wide-ranging strategy that can utilize a variety of cationic metal species. In a similar manner, we envision a complementary strategy using chiral cation in partnership with inorganic anionic metal salts. Herein, we report a chiral dicationic bisguanidinium-catalyzed asym. oxidation reaction of alkenes with potassium permanganate. Chiral induction is attributed to ion-pairing interaction between chiral cation and enolate anion. The success of the current permanganate oxidation reaction together with mechanistic insights should provide inspiration for expansion to other anionic metal salts and would open up new paradigms for asym. transition metal catalysis, phase-transfer catalysis, and ion-pairing catalysis. Thus, e.g., dihydroxylation of tert-Bu 2-phenylacrylate with KMnO₄ in presence of biguanidinium I.2Cl^–/KI afforded diol II (65% yield, 92% ee). In the experiment, the researchers used many compounds, for example, Isopentyltriphenylphosphonium bromide (cas: 28322-40-9HPLC of Formula: 28322-40-9).

Isopentyltriphenylphosphonium bromide (cas: 28322-40-9) 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.HPLC of Formula: 28322-40-9

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Organophosphorus compounds. 109. Synthesis of fluorescent reagents with chemically selective anchor groups was written by Horner, Leopold;Hallenbach, Werner. And the article was included in Phosphorus and Sulfur and the Related Elements in 1984.Name: 1-Bromo-4-methoxybutane This article mentions the following:

About 20 title compounds were prepared Thus acridine was alkylated with RO(CH₂)_nLi (R = Me, Et, tetrahydropyranyl; n = 3, 4, 6) to give dihydroacridines I, which were oxidized to give alkylacridines II (R¹ = OMe, OEt, OH). II (R¹ = OH; n = 2, 3, 4, 6) reacted with ClP(O)MeR² (R² = OEt, F) to give II [R¹ = OP(O)MeR²]. II [R¹ = OP(O)MeF, n = 4] and serine derivative HOCH₂CH(CO₂H)NHCO₂CMe₃ gave II [R¹ = OP(O)MeOCH₂CH(CO₂H)NHCO₂CMe₃]. Bromoalkylacridines II (R¹ = Br; n = 2, 3, 4, 6) and NaP(O)(OR³)₂ (R³ = Et, Bu) gave II [R¹ = P(O)(OR³)₂]. In the experiment, the researchers used many compounds, for example, 1-Bromo-4-methoxybutane (cas: 4457-67-4Name: 1-Bromo-4-methoxybutane).

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

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary