Category: bromides-buliding-blocks

Slack, Eric D.; Colacot, Thomas J. published the artcile< Understanding the Activation of Air-Stable Ir(COD)(Phen)Cl Precatalyst for C-H Borylation of Aromatics and Heteroaromatics>, Synthetic Route of 401-78-5, the main research area is iridium complex catalyzed carbon hydrogen bond borylation aromatic heteroaromatic; borane aromatic heteroaromatic derivative preparation.

A newly developed robust catalyst [Ir(COD)(Phen)Cl] (A) was used for the C-H borylation of three dozen aromatics and heteroaromatics with excellent yield and selectivity. Activation of the catalyst was identified using catalytic amounts of H2O, alcs., etc., when B2pin2 was used in noncoordinating solvents, while for THF catalytic use of HBpin was required. The results were on par with the in situ based expensive system [Ir(OMe)(COD)]2/dtbbpy or Me4Phen.

Organic Letters published new progress about Aromatic compounds Role: RCT (Reactant), RACT (Reactant or Reagent). 401-78-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4BrF3, Synthetic Route of 401-78-5.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Zhou, Bing; Hu, Jiantao; Xu, Fuming; Chen, Zhuo; Bai, Longchuan; Fernandez-Salas, Ester; Lin, Mei; Liu, Liu; Yang, Chao-Yie; Zhao, Yujun; McEachern, Donna; Przybranowski, Sally; Wen, Bo; Sun, Duxin; Wang, Shaomeng published the artcile< Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression>, SDS of cas: 337536-14-8, the main research area is preparation degrader bromodomain extra terminal protein cancer.

The bromodomain and extra-terminal (BET) family proteins, consisting of BRD2, BRD3, BRD4, and testis-specific BRDT members, are epigenetic “”readers”” and play a key role in the regulation of gene transcription. BET proteins are considered to be attractive therapeutic targets for cancer and other human diseases. Recently, heterobifunctional small-mol. BET degraders have been designed based upon the proteolysis targeting chimera (PROTAC) concept to induce BET protein degradation Herein, we present our design, synthesis, and evaluation of a new class of PROTAC BET degraders. One of the most promising compounds, 23, effectively degrades BRD4 protein at concentrations as low as 30 pM in the RS4;11 leukemia cell line, achieves an IC50 value of 51 pM in inhibition of RS4;11 cell growth and induces rapid tumor regression in vivo against RS4;11 xenograft tumors. These data establish that compound 23 (BETd-260/ZBC260) is a highly potent and efficacious BET degrader.

Journal of Medicinal Chemistry published new progress about Antiproliferative agents. 337536-14-8 belongs to class bromides-buliding-blocks, and the molecular formula is C9H8Br2O2, SDS of cas: 337536-14-8.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Doerner, Bernd; Kuntner, Claudia; Bankstahl, Jens P.; Wanek, Thomas; Bankstahl, Marion; Stanek, Johann; Muellauer, Julia; Bauer, Florian; Mairinger, Severin; Loescher, Wolfgang; Miller, Donald W.; Chiba, Peter; Mueller, Markus; Erker, Thomas; Langer, Oliver published the artcile< Radiosynthesis and in vivo evaluation of 1-[18F]fluoroelacridar as a positron emission tomography tracer for P-glycoprotein and breast cancer resistance protein>, COA of Formula: C7H4BrNO4, the main research area is fluorine 18 elacridar preparation PET tumor imaging Pgp BCRP.

Aim of this study was to label the potent dual P-glycoprotein (Pgp) and breast cancer resistance protein (BCRP) inhibitor elacridar (1) with 18F to provide a positron emission tomog. (PET) radiotracer to visualize Pgp and BCRP. A series of new 1- and 2-halogen- and nitro-substituted derivatives of 1 (4a-e) was synthesized as precursor mols. and reference compounds for radiolabelling and shown to display comparable in vitro potency to 1 in increasing rhodamine 123 accumulation in a cell line overexpressing human Pgp (MDCKII-MDR1). 1-[18F]fluoroelacridar ([18F]4b) was synthesized in a decay-corrected radiochem. yield of 1.7 ± 0.9% by a 1-step no-carrier added nucleophilic aromatic 18F-substitution of 1-nitro precursor 4c. Small-animal PET imaging of [18F]4b was performed in naive rats, before and after administration of unlabeled 1 (5 mg/kg, n = 3), as well as in wild-type and Mdr1a/b (-/-) Bcrp1 (-/-) mice (n = 3). In PET experiments in rats, administration of unlabeled 1 increased brain activity uptake by a factor of 9.5 (p = 0.0002, 2-tailed Student’s t-test), whereas blood activity levels remained unchanged. In Mdr1a/b (-/-) Bcrp1 (-/-) mice, the mean brain-to-blood ratio of activity at 60 min after tracer injection was 7.6 times higher as compared to wild-type animals (p = 0.0002). HPLC anal. of rat brain tissue extracts collected at 40 min after injection of [18F]4b revealed that 93 ± 7% of total radioactivity in brain was in the form of unchanged [18F]4b. In conclusion, the in vivo behavior of [18F]4b was found to be similar to previously described [11C]1 suggesting transport of [18F]4b by Pgp and/or BCRP at the rodent BBB. However, low radiochem. yields and a significant degree of in vivo defluorination will limit the utility of [18F]4b as a PET tracer.

Bioorganic & Medicinal Chemistry published new progress about Animal gene, MDR1 Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 16426-64-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4BrNO4, COA of Formula: C7H4BrNO4.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Cao, Feng-Xia; Zhao, Li-Ming published the artcile< Cyclization of 1,4-dihydroxyanthraquinone with α,β-unsaturated aldehyde: a new strategy for the synthesis of cyclopentanoids>, Category: bromides-buliding-blocks, the main research area is cyclopentanoid preparation dihydroxyanthraquinone cyclization alpha beta unsaturated aldehyde.

A cascade cyclization strategy was developed for the synthesis of cyclopentane-fused anthraquinones through the condensation of 1,4-dihydroxyanthraquinone with α,β-unsaturated aldehydes in the presence of common inorganic base NaOH. These fused-tetracyclic anthraquinone products are formed in a single step from readily accessible starting materials under very mild conditions without the use of any expensive or complex reagents. This method represents an unprecedented example of a base-promoted protocol to access five-membered carbocyclic rings in a single step. Moreover, this chem. also provides useful guidance for the preparation of 6,5-fused ring systems.

Tetrahedron Letters published new progress about Crystal structure. 3893-18-3 belongs to class bromides-buliding-blocks, and the molecular formula is C9H7BrO, Category: bromides-buliding-blocks.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Brandstatter, Marco; Huwyler, Nikolas; Carreira, Erick M. published the artcile< Gold(I)-catalyzed stereoselective cyclization of 1,3-enyne aldehydes by a 1,3-acyloxy migration/Nazarov cyclization/aldol addition cascade>, COA of Formula: C21H22BrP, the main research area is bicyclooctenone preparation diastereoselective enantioselective; enyne aldehyde propargylic acetate preparation cyclization tandem gold catalyst.

Stereoselective synthesis of bicyclo[3.3.0]octenones I (R = Ph, naphthalen-2-yl, i-Pr, etc.) from chiral 1,3-enyne aldehydes bearing propargylic acetates (R,E/Z)-CH3CH(OC(O)CH3)CCC(R)=CH(CH2)2CHO is described. The method is based on a Au(I)-catalyzed domino sequence with concomitant transfer of chirality involving 1,3-acyloxy migration followed by Nazarov cyclization and an unprecedented aldol addition The method furnishes densely functionalized bicyclic structures in high yields, with up to 97% ee and good diastereoselectivity.

Chemical Science published new progress about Aldol addition catalysts, stereoselective. 1530-33-2 belongs to class bromides-buliding-blocks, and the molecular formula is C21H22BrP, COA of Formula: C21H22BrP.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Lin, Xia; Fang, Chengtao; Huang, Xiaolei; Xiao, Xiaohui published the artcile< 1,1,2-Tribromoethyl arenes: novel and highly efficient precursors for the synthesis of 1-bromoalkynes and α-bromoketones>, Computed Properties of 2725-82-8, the main research area is bromoalkyne bromoketone preparation; tribromoethyl arene preparation elimination reaction; ethylbenzene bromination.

Herein, a novel method to synthesize 1,1,2-tribromoethyl arenes, which can be easily transformed to 1-bromoalkynes via base-mediated elimination reaction is reported. The bromination reagent was in situ generated from the reaction of NaBr/NaBrO3/H2SO4, resulting in high reactivity, excellent chem. selectivity and outstanding functional group tolerance. Moreover, 1,1,2-tribromoethyl arenes encounter a selectivity switch to afford α-bromoketones under strong acidic conditions.

Organic Chemistry Frontiers published new progress about Alkynes, bromo Role: SPN (Synthetic Preparation), PREP (Preparation). 2725-82-8 belongs to class bromides-buliding-blocks, and the molecular formula is C8H9Br, Computed Properties of 2725-82-8.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Mondal, B.; Bendikov, M.; Kanti Roy, U. published the artcile< Oligoselenophenes (n and p Type): Synthesis and Properties>, Category: bromides-buliding-blocks, the main research area is oligoselenophene preparation semiconductor thermal property.

An array of semiconducting oligoselenophenes (n and p types), up to hexamer units, e.g., I were synthesized by the double Stille coupling methods using tetrakis(triphenylphosphine)palladium(0) as a catalyst. A series of semiconducting oligomers (n and p types) containing mixed hetero-units (hexamers of thiophene and selenophene), e.g., II were also synthesized using the Stille coupling reaction. Their thermal properties were systematically studied and compared with those of π-conjugated thiophene based oligomers using DSC and TGA. The field-effect mobility of synthesized n and p type oligomers was analyzed.

Russian Journal of General Chemistry published new progress about Selenides Role: PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation) (cyclic). 3480-11-3 belongs to class bromides-buliding-blocks, and the molecular formula is C8H5BrS2, Category: bromides-buliding-blocks.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Matsui, Y; Figi, A; Horikawa, M; Jahangiri Noudeh, Y; Tomozawa, Y; Hashimoto, K; Kaufman, J A; Farsad, K published the artcile< Erratum to ""Arteriopathy after transarterial chemo-lipiodolization for hepatocellular carcinoma"" [Diagn. Interv. Imaging 98 (12) (2017) 827-35].>, Name: 4-Bromoisobenzofuran-1,3-dione, the main research area is .

There is no abstract available for this document.

Diagnostic and interventional imaging published new progress about 82-73-5. 82-73-5 belongs to class bromides-buliding-blocks, and the molecular formula is C8H3BrO3, Name: 4-Bromoisobenzofuran-1,3-dione.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Song, Jing-Ru; Li, Na; Li, Dian-Peng published the artcile< Synthesis and anti-proliferation activity of Mogrol derivatives bearing quinoline and triazole moieties>, Related Products of 29124-57-0, the main research area is Mogrol quinolinyl triazolyl synthesis antitumor agent; Lung cancer; Mogrol; Quinoline; Structural modification; Triazole.

A series of novel derivatives based on Mogrol were designed and synthesized in attempt to improve anti-lung cancer activity. The cytotoxicity against human lung cancer cells including A549 and NCI-H460 were performed by Cell Counting Kit-8 (CCK8) assay in vitro. The screening result showed that compound 8f exhibited the strongest activity with an IC50 value of 4.47μM against A549 cell, and could induce the cell apoptosis in a dose-dependent manner and arrest cell cycle at G0/G1 phase. Besides, compound 8f displayed anti-proliferation effect on A549 cell through inhibiting phosphorylation of signal transducer and activator of transcription 3 (STAT3). Furthermore, compared with Mogrol, compound 10a significantly improved the cytotoxicity against NCI-H460 with the IC50 value of 17.13μM. The research stimulated the development of potential therapeutic agent for lung cancer from the natural Mogrol.

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 29124-57-0 belongs to class bromides-buliding-blocks, and the molecular formula is C7H6BrNO, Related Products of 29124-57-0.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Pocinho, Alexandre; Mallet-Ladeira, Sonia; Hureau, Christelle; Gras, Emmanuel published the artcile< N,N′-Bis(4-bromophenyl)-N,N′-dimethylurea>, Quality Control of 639520-70-0, the main research area is bisbromophenyl dimethylurea preparation crystal structure.

The structure of the title compound, C15H14Br2N2O, at 180 K has monoclinic (P21/n) symmetry. It was obtained unexpectedly from the decomposition of the parent 4-bromo-N-tert-butoxycarbonyl-N-methyl-aniline. It exhibits an ′endo′ conformation with angles between the two aromatic rings slightly lower than the average values found for similar compounds on the Cambridge Structural Database. In the crystal, C-H···O hydrogen bonds and short Br···Br halogen bonds [3.444 (1) Å] are observed

IUCrData published new progress about Crystal structure. 639520-70-0 belongs to class bromides-buliding-blocks, and the molecular formula is C12H16BrNO2, Quality Control of 639520-70-0.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary