Category: 76283-09-5

In 2022,Marine Drugs included an article by Chao, Rong; Said, Gulab; Zhang, Qun; Qi, Yue-Xuan; Hu, Jie; Zheng, Cai-Juan; Zheng, Ji-Yong; Shao, Chang-Lun; Chen, Guang-Ying; Wei, Mei-Yan. SDS of cas: 76283-09-5. The article was titled 《Design, Semisynthesis, Insecticidal and Antibacterial Activities of a Series of Marine-Derived Geodin Derivatives and Their Preliminary Structure-Activity Relationships》. The information in the text is summarized as follows:

To enhance the biol. activity of the natural product geodin isolated from the marine-derived fungus Aspergillus sp., a series of new ether derivatives I [R = Et, 2-bromobenzyl, 2-chlorobenzyl, etc.] was designed and semisynthesized using a high-yielding one-step reaction. In addition, the insecticidal and antibacterial activities of all geodin congeners I were evaluated systematically. Most of these derivatives I showed better insecticidal activities against Helicoverpa armigera Hubner than Geodin. In particular, I [R = 2,3,4,5-tetrafluorobenzyl] showed potent insecticidal activity with an IC50 value of 89μM, comparable to the pos. control azadirachtin (IC50 = 70μM). Addnl., I [R = 2-chlorobenzyl, 2-fluorobenzyl, 3,5-difluorobenzyl, 2,3,4-trifluorobenzyl, 4-cyanobenzyl and 2-fluoro-3-chlorobenzyl] showed strong antibacterial activity against Staphylococcus aureus and Aeromonas salmonicida with MIC values in the range of 1.15-4.93μM. The preliminary structure-activity relationships indicated that the introduction of halogenated benzyl especially fluorobenzyl, into geodin and substitution of 4-OH was a key factors in increasing the insecticidal and antibacterial activities of geodin. The experimental process involved the reaction of 4-Bromo-1-(bromomethyl)-2-fluorobenzene(cas: 76283-09-5SDS of cas: 76283-09-5)

4-Bromo-1-(bromomethyl)-2-fluorobenzene(cas: 76283-09-5) 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. SDS of cas: 76283-09-5 In contrast, terrestrial plants account only for a few bromine-containing compounds.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

《Dipolar HCP materials as alternatives to DMF solvent for azide-based synthesis》 was published in Green Chemistry in 2021. These research results belong to Gao, Feng; Bai, Rongxian; Li, Minghao; Gu, Yanlong. Electric Literature of C7H5Br2F The article mentions the following:

Hypercrosslinked polymers HCP-DMF and HCP-DMF-SO3H containing abundant and flexible DMF moieties were designed and synthesized. Benefitting from the solvation microenvironment provided by the pseudo-DMF moities, the polar HCPs manifested outstanding performances in the conversions of NaN3 to benzylic azides and 1,2,3-triazoles in EtOH (95%), resp., avoiding the use of risky DMF and improving the separation processes of the products. The experimental part of the paper was very detailed, including the reaction process of 4-Bromo-1-(bromomethyl)-2-fluorobenzene(cas: 76283-09-5Electric Literature of C7H5Br2F)

4-Bromo-1-(bromomethyl)-2-fluorobenzene(cas: 76283-09-5) 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. Electric Literature of C7H5Br2F

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Category: bromides-buliding-blocksOn June 5, 2020, Li, Ya-Wei; Zheng, Hong-Xing; Yang, Bo; Shan, Xiang-Huan; Qu, Jian-Ping; Kang, Yan-Biao published an article in Organic Letters. The article was 《tBuOK-Promoted Cyclization of Imines with Aryl Halides》. The article mentions the following:

A transition-metal-free indole synthesis using radical coupling of 2-halotoluenes and imines via the later-stage C-N bond construction was reported for the first time. It includes an aminyl radical generation by C-H cleaving addition of 2-halotoluenes to imines via the carbanion radical relay and an intramol. coupling of aryl halides with aminyl radicals. One standard condition can be used for all halides including F, Cl, Br, and I. No extra oxidant or transition metal is required. In the experiment, the researchers used 4-Bromo-1-(bromomethyl)-2-fluorobenzene(cas: 76283-09-5Category: bromides-buliding-blocks)

4-Bromo-1-(bromomethyl)-2-fluorobenzene(cas: 76283-09-5) belongs to organobromine compounds.The reactivity of organobromine compounds resembles but is intermediate between the reactivity of organochlorine and organoiodine compounds. Dehydrobromination, Grignard reactions, reductive coupling, Wittig reaction, and several nucleophilic substitution reactions are some of the principal reactions which involve organic bromides.Category: bromides-buliding-blocks

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Electric Literature of C7H5Br2FOn September 16, 2021 ,《Structure-Activity Relationship and Mode-of-Action Studies Highlight 1-(4-Biphenylylmethyl)-1H-imidazole-Derived Small Molecules as Potent CYP121 Inhibitors》 was published in ChemMedChem. The article was written by Walter, Isabell; Adam, Sebastian; Gentilini, Maria Virginia; Kany, Andreas M.; Brengel, Christian; Thomann, Andreas; Sparwasser, Tim; Kohnke, Jesko; Hartmann, Rolf W.. The article contains the following contents:

CYP121 of Mycobacterium tuberculosis (Mtb) is an essential target for the development of novel potent drugs against tuberculosis (TB). Besides known antifungal azoles, further compounds of the azole class were recently identified as CYP121 inhibitors with antimycobacterial activity. Herein, we report the screening of a similarity-oriented library based on the former hit compound, the evaluation of affinity toward CYP121, and activity against M. bovis BCG. The results enabled a comprehensive SAR study, which was extended through the synthesis of promising compounds and led to the identification of favorable features for affinity and/or activity and hit compounds with 2.7-fold improved potency. Mode of action studies show that the hit compounds inhibit substrate conversion and highlighted CYP121 as the main antimycobacterial target of our compounds Exemplified complex crystal structures of CYP121 with three inhibitors reveal a common binding site. Engaging in both hydrophobic interactions as well as hydrogen bonding to the sixth iron ligand, our compounds block a solvent channel leading to the active site heme. Addnl., we report the first CYP inhibitors that are able to reduce the intracellular replication of M. bovis BCG in macrophages, emphasizing their potential as future drug candidates against TB. In the experimental materials used by the author, we found 4-Bromo-1-(bromomethyl)-2-fluorobenzene(cas: 76283-09-5Electric Literature of C7H5Br2F)

4-Bromo-1-(bromomethyl)-2-fluorobenzene(cas: 76283-09-5) belongs to organobromine compounds.Depending on the type of carbon to which the bromine is bonded, organic bromide could be alkyl, alkenyl, alkynyl, or aryl. Dehydrobromination, Grignard reactions, reductive coupling, Wittig reaction, and several nucleophilic substitution reactions are some of the principal reactions which involve organic bromides. Electric Literature of C7H5Br2F

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

In 2019,Chemical Science included an article by Cheng, Cang; Wan, Bin; Zhou, Bo; Gu, Yichao; Zhang, Yanghui. Reference of 4-Bromo-1-(bromomethyl)-2-fluorobenzene. The article was titled 《Enantioselective synthesis of quaternary 3,4-dihydroisoquinolinones via Heck carbonylation reactions: development and application to the synthesis of Minalrestat analogues》. The information in the text is summarized as follows:

Minalrestat and its analogs represent structurally novel aldose reductase inhibitors, and the asym. synthesis of such pharmaceutically privileged mols. has not been reported yet. We have developed a palladium-catalyzed enantioselective intramol. carbonylative Heck reaction by using formate esters as the source of CO, which represents the first enantioselective synthesis of quaternary 3,4-dihydroisoquinolines. The reaction provides a facile and efficient method for the synthesis of enantiopure nitrogen-containing heterocyclic compounds bearing an all-carbon quaternary stereocenter. The reaction has been successfully applied to the first asym. synthesis of Minalrestat analogs. The experimental part of the paper was very detailed, including the reaction process of 4-Bromo-1-(bromomethyl)-2-fluorobenzene(cas: 76283-09-5Reference of 4-Bromo-1-(bromomethyl)-2-fluorobenzene)

4-Bromo-1-(bromomethyl)-2-fluorobenzene(cas: 76283-09-5) 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. Reference of 4-Bromo-1-(bromomethyl)-2-fluorobenzene

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Brem, Jurgen; Panduwawala, Tharindi; Hansen, Jon Ulf; Hewitt, Joanne; Liepins, Edgars; Donets, Pawel; Espina, Laura; Farley, Alistair J. M.; Shubin, Kirill; Campillos, Gonzalo Gomez; Kiuru, Paula; Shishodia, Shifali; Krahn, Daniel; Lesniak, Robert K.; Schmidt, Juliane; Calvopina, Karina; Turrientes, Maria-Carmen; Kavanagh, Madeline E.; Lubriks, Dmitrijs; Hinchliffe, Philip; Langley, Gareth W.; Aboklaish, Ali F.; Eneroth, Anders; Backlund, Maria; Baran, Andrei G.; Nielsen, Elisabet I.; Speake, Michael; Kuka, Janis; Robinson, John; Grinberga, Solveiga; Robinson, Lindsay; McDonough, Michael A.; Rydzik, Anna M.; Leissing, Thomas M.; Jimenez-Castellanos, Juan Carlos; Avison, Matthew B.; Da Silva Pinto, Solange; Pannifer, Andrew D.; Martjuga, Marina; Widlake, Emma; Priede, Martins; Hopkins Navratilova, Iva; Gniadkowski, Marek; Belfrage, Anna Karin; Brandt, Peter; Yli-Kauhaluoma, Jari; Bacque, Eric; Page, Malcolm G. P.; Bjorkling, Fredrik; Tyrrell, Jonathan M.; Spencer, James; Lang, Pauline A.; Baranczewski, Pawel; Canton, Rafael; McElroy, Stuart P.; Jones, Philip S.; Baquero, Fernando; Suna, Edgars; Morrison, Angus; Walsh, Timothy R.; Schofield, Christopher J. published an article on January 31 ,2022. The article was titled 《Imitation of β-lactam binding enables broad-spectrum metallo-β-lactamase inhibitors》, and you may find the article in Nature Chemistry.Formula: C7H5Br2F The information in the text is summarized as follows:

Carbapenems are vital antibiotics, but their efficacy is increasingly compromised by metallo-β-lactamases (MBLs). Here we report the discovery and optimization of potent broad-spectrum MBL inhibitors. A high-throughput screen for NDM-1 inhibitors identified indole-2-carboxylates (InCs) as potential β-lactamase stable β-lactam mimics. Subsequent structure-activity relationship studies revealed InCs as a new class of potent MBL inhibitor, active against all MBL classes of major clin. relevance. Crystallog. studies revealed a binding mode of the InCs to MBLs that, in some regards, mimics that predicted for intact carbapenems, including with respect to maintenance of the Zn(II)-bound hydroxyl, and in other regards mimics binding observed in MBL-carbapenem product complexes. InCs restore carbapenem activity against multiple drug-resistant Gram-neg. bacteria and have a low frequency of resistance. InCs also have a good in vivo safety profile, and when combined with meropenem show a strong in vivo efficacy in peritonitis and thigh mouse infection models. [graphic not available: see fulltext] The experimental part of the paper was very detailed, including the reaction process of 4-Bromo-1-(bromomethyl)-2-fluorobenzene(cas: 76283-09-5Formula: C7H5Br2F)

4-Bromo-1-(bromomethyl)-2-fluorobenzene(cas: 76283-09-5) belongs to organobromine compounds.Depending on the type of carbon to which the bromine is bonded, organic bromide could be alkyl, alkenyl, alkynyl, or aryl. Formula: C7H5Br2F Alkyl bromides are mainly used as alkylating agents and also find application as a solvent to extract oil from seeds and wool.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

《Development of pyrazolo[3,4-d]pyrimidine-6-amine-based TRAP1 inhibitors that demonstrate in vivo anticancer activity in mouse xenograft models》 was written by Kim, Darong; Kim, So-Yeon; Kim, Dongyoung; Yoon, Nam Gu; Yun, Jisu; Hong, Ki Bum; Lee, Changwook; Lee, Ji Hoon; Kang, Byoung Heon; Kang, Soosung. Quality Control of 4-Bromo-1-(bromomethyl)-2-fluorobenzene And the article was included in Bioorganic Chemistry on August 31 ,2020. The article conveys some information:

TNF Receptor Associated Protein 1 (TRAP1) is a mitochondrial paralog of Hsp90 related to the promotion of tumorigenesis in various cancers via maintaining mitochondrial integrity, reducing the production of reactive oxygen species, and reprogramming cellular metabolism Consequently, Hsp90 and TRAP1 have been targeted to develop cancer therapeutics. Herein, we report a series of pyrazolo[3,4-d]pyrimidine derivatives that are mitochondria-permeable TRAP1 inhibitors. Structure-based drug design guided the optimization of potency, leading to the identification of compounds 47 and 48 as potent TRAP1 and Hsp90 inhibitors with good metabolic and plasma stability as well as acceptable CYP and hERG inhibition. X-ray co-crystallization studies confirmed both 47 and 48 interact with the ATP binding pocket in the TRAP1 protein. Compounds 47 and 48 demonstrated excellent anticancer efficiency in various cancer cells, with limited toxicity over normal hepatocyte and prostate cells. Mouse PC3 xenograft studies showed 47 and 48 significantly reduced tumor growth. The experimental process involved the reaction of 4-Bromo-1-(bromomethyl)-2-fluorobenzene(cas: 76283-09-5Quality Control of 4-Bromo-1-(bromomethyl)-2-fluorobenzene)

4-Bromo-1-(bromomethyl)-2-fluorobenzene(cas: 76283-09-5) belongs to organobromine compounds.Organobromine chemicals are produced naturally by an array of biological and other chemical processes in our environment. Organobromine compounds are produced naturally by marine creatures (sponges, corals, sea slugs, tunicates, sea fans) and seaweed, plants, fungi, lichen, algae, bacteria, microbes, and some mammals. Quality Control of 4-Bromo-1-(bromomethyl)-2-fluorobenzene

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary