Category: 16426-64-5

Kan, Jian; Huang, Shijun; Lin, Jin; Zhang, Min; Su, Weiping published the artcile< Silver-Catalyzed Arylation of (Hetero)arenes by Oxidative Decarboxylation of Aromatic Carboxylic Acids>, Synthetic Route of 16426-64-5, the main research area is carboxylic acid aromatic oxidative decarboxylative coupling Minisci arene heteroarene; biaryl preparation; CH activation; heterocycles; oxidation; radicals; silver.

The silver-catalyzed intermol. Minisci-type reaction of aromatic carboxylic acids was developed. With an inexpensive silver salt as a catalyst, this new reaction enabled a variety of aromatic carboxylic acids R1CO2H (R1 = 4-NCC6H4, 3-BrC6H4, 2-Cl-4-MeSO2C6H3, 2-chloro-3-pyridyl, etc.) to undergo decarboxylative coupling with electron-deficient arenes or heteroarenes R2H (R2 = Ph, 2,5-F2C6H3, pyridyl, etc.) regardless of the position of the substituents on the aromatic carboxylic acid, thus eliminating the need for ortho-substituted aromatic carboxylic acids, which were a limitation of previously reported methods.

Angewandte Chemie, International Edition published new progress about Aromatic carboxylic acids Role: RCT (Reactant), RACT (Reactant or Reagent). 16426-64-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4BrNO4, Synthetic Route of 16426-64-5.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Bernard, Alimenla; Kumar, Anil; Jamir, Latonglila; Sinha, Dipak; Sinha, Upasana Bora published the artcile< An efficient microwave-induced solvent-free organic bromination using tetrabutylammonium tribromide>, Reference of 16426-64-5, the main research area is arene bromination tetrabutylammonium tribromide microwave irradiation solventless; bromo arene preparation; organic substrate bromination tetrabutylammonium tribromide microwave irradiation solventless; brominated compound preparation; tetrabutylammonium tribromide solventless bromination reagent; microwave irradiation solventless bromination mediator.

Microwave-induced solvent-free brominations of organic substrates have been carried out with tetrabutylammonium tribromide, (C4H9)4N+(Br3-). Reaction procedure was facile, affording products in high yields within very short reaction times.

Acta Chimica Slovenica published new progress about Aromatic hydrocarbons Role: RCT (Reactant), RACT (Reactant or Reagent). 16426-64-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4BrNO4, Reference of 16426-64-5.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Wu, Pu Hua; Meng, Qing Qing; Zhou, Hu Chen published the artcile< Synthesis of a novel pyrrolo-benzoxaborole scaffold and its derivatization via Friedel-Crafts reaction catalyzed by anhydrous stannic chloride>, Recommanded Product: 2-Bromo-4-nitrobenzoic acid, the main research area is pyrrolobenzoxaborole preparation Friedel Crafts acylation acyl chloride stannic catalyst; acyl pyrrolobenzoxaborole preparation.

A novel pyrrolo-benzoxaborole, 6-(pyrrol-1-yl)-1,3-dihydro-1-hydroxy-2,1-benzoxaborole, was synthesized with 27% overall yield over six steps from 2-bromo-1-methyl-4-nitrobenzene as starting material. Its derivation was achieved via Friedel-Crafts reaction catalyzed by anhydrous stannic chloride with various acyl chlorides giving 3-acyl-1-phenylpyrroles as the main products.

Chinese Chemical Letters published new progress about Acid chlorides Role: RCT (Reactant), RACT (Reactant or Reagent). 16426-64-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4BrNO4, Recommanded Product: 2-Bromo-4-nitrobenzoic acid.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Singh, Sudhir K.; Ruchelman, Alexander L.; Li, Tsai-Kun; Liu, Angela; Liu, Leroy F.; LaVoie, Edmond J. published the artcile< Nitro and Amino Substitution in the D-Ring of 5-(2-Dimethylaminoethyl)- 2,3-methylenedioxy-5H-dibenzo[c,h][1,6]naphthyridin-6-ones: Effect on Topoisomerase-I Targeting Activity and Cytotoxicity>, Application of C7H4BrNO4, the main research area is methylenedioxydibenzonaphthyridinone preparation topoisomerase inhibiting activity cytotoxicity; structure methylenedioxydibenzonaphthyridinone topoisomerase inhibiting activity cytotoxicity; nitro amino substitution methylenedioxydibenzonaphthyridinone topoisomerase targeting activity cytotoxicity.

Methylenedioxydibenzo[c,h][1,6]naphthyridinones I (R, R1, R2 = H, H2N, O2N; R3 = Me2N, Et) are prepared as potential inhibitors of human topoisomerase I. Coupling of 2-bromobenzoic acids to amino(methylenedioxy)quinolines [prepared by displacement of 4-chloro-6,7-(methylenedioxy)quinoline] followed by palladium-catalyzed intramol. Heck arylation reactions and reduction of the pendant nitro groups (if present) yields methylenedioxydibenzonaphthyridinones I (R, R1, R2 = H, H2N, O2N; R3 = Me2N, Et). I (R = H; R1 = H, O2N; R2 = O2N, H; R3 = Me2N) inhibit topoisomerase I-mediated DNA cleavage more effectively and are more cytotoxic than camptothecin; I have topoisomerase I inhibiting activities comparable to dimethoxydibenzonaphthyridinone I (R = H; R1 = R2 = MeO; R3 = Me2N).

Journal of Medicinal Chemistry published new progress about Cytotoxic agents. 16426-64-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4BrNO4, Application of C7H4BrNO4.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Huang, Wenyi; Shrestha, Mohini; Wang, Chenchen; Fang, Ke; Teng, Yaxin; Qu, Jingping; Chen, Yifeng published the artcile< Asymmetric synthesis of 3-benzyl and allyl isoindolinones by Pd-catalyzed dicarbofunctionalization of 1,1-disubstituted enamides>, Application of C7H4BrNO4, the main research area is disubstituted isoindolinone enantioselective preparation; boronic acid disubstituted enamide tandem Heck Suzuki palladium catalyst.

A palladium-catalyzed asym. synthesis of 3,3-disubstituted isoindolinones I [R = (E)-n-BuCH=CH, 3-thienyl, PMB, etc.; R1 = Bn, (CH2)2Ph, PMB; R2 = Me, iPr; R3 = H, 6-Cl, 5-NO2; etc.] via tandem Heck/Suzuki coupling of 1,1-disubstituted enamides with aryl/alkenyl boronic acids under mild reaction conditions was reported. This reaction exhibited both broad functional group tolerance and high enantioselectivity. The first dicarbo-functionalization of 1,1-disubstituted enamides to generate amide derivatives bearing quaternary stereocenters was reported. Finally, synthetic utility of this protocol was demonstrated by expedient synthesis of PI3K-delta inhibitor precursor.

Organic Chemistry Frontiers published new progress about Amides Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation) (enamides). 16426-64-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4BrNO4, Application of C7H4BrNO4.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Yu, Peng; Hu, Jun; Wan, Rong; Li, Xi; Zheng, Shanlong; Xu, Yanhua published the artcile< Synthesis of N-(5-aryl-1,3,4-thiadiazol-2-yl)-2-(3-oxo-1,2-benzothiazol-2(3H)-yl)acetamide derivatives promoted by carbodiimide condensation>, HPLC of Formula: 16426-64-5, the main research area is benzoic acid thiosemicarbazide heterocyclization; thiadiazole preparation single crystal benzisothiazolinone condensation carbodiimide catalyst; acetamide preparation.

Novel N-(5-aryl-1,3,4-thiadiazol-2-yl)-2-(3-oxo-1,2-benzothiazol-2(3H)-yl)acetamide derivatives I [R = H, 3-CH3, 4-Cl, 2-Br, etc.] were prepared by 2-amino-5-substituted phenyl-1,3,4-thiadiazole and 2-(3-oxo-1,2-benzothiazol-2(3H)-yl) acetic acid condensation catalysis in a convenient and fast method. The intermediate compound 5-(2-chlorophenyl)-1,3,4-thiadiazol-2-amine was confirmed by single-crystal X-ray diffraction.

Journal of Chemical Research published new progress about Amides Role: SPN (Synthetic Preparation), PREP (Preparation). 16426-64-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4BrNO4, HPLC of Formula: 16426-64-5.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Carrico, Dora; Ohkanda, Junko; Kendrick, Howard; Yokoyama, Kohei; Blaskovich, Michelle A.; Bucher, Cynthia J.; Buckner, Frederick S.; Van Voorhis, Wesley C.; Chakrabarti, Debopam; Croft, Simon L.; Gelb, Michael H.; Sebti, Said M.; Hamilton, Andrew D. published the artcile< In vitro and in vivo antimalarial activity of peptidomimetic protein farnesyltransferase inhibitors with improved membrane permeability>, Computed Properties of 16426-64-5, the main research area is FRI2148 prodrug preparation antimalarial Plasmodium farnesyltransferase inhibitor.

A series of protein farnesyltransferase inhibitor ester prodrugs of FTI-2148 were synthesized in order to evaluate the effects of ester structure modification on antimalarial activity and for further development of a farnesyltransferase inhibitor with in vivo activity. Evaluation against P. falciparum in red blood cells showed that all the investigated esters exhibited significant antimalarial activity, with the benzyl ester 16 showing the best inhibition (ED50 = 150 nM). Addnl., compound I displayed in vivo activity and was found to suppress parasitemia by 46.1% at a dose of 50 mg kg-1 day-1 against Plasmodium berghei in mice. The enhanced inhibition potency of the esters is consistent with improved cell membrane permeability compared to that of the free acid. The results of this study suggest that protein farnesyltransferase is a valid antimalarial drug target and that the antimalarial activity of these compounds derives from a balance between the hydrophobic character and the size and conformation of the ester moiety.

Bioorganic & Medicinal Chemistry published new progress about Antimalarials. 16426-64-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4BrNO4, Computed Properties of 16426-64-5.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Jin, Cong-Yang; Du, Ji-Yuan; Zeng, Chao; Zhao, Xian-He; Cao, Ye-Xing; Zhang, Xiang-Zhi; Lu, Xin-Yun; Fan, Chun-An published the artcile< Hypervalent iodine(III)-mediated oxidative dearomatizing cyclization of arylamines>, Application In Synthesis of 16426-64-5, the main research area is amido aryl amine iodane mediated oxidative dearomatizing spirocyclization; spiro lactam cyclohexadiene iminium preparation.

An oxidative dearomatizing cyclization of aryl amines promoted by iodobenzene bis(trifluoroacetate) [PhI(CF3CO2)2] was explored, leading to a novel synthetic approach to functionalized spirocyclic building blocks containing a structurally unique dieniminium moiety. This unprecedented methodol., featuring oxidative dearomatization and carbon-carbon bond-forming cyclization, to some extent, not only expands the synthetic potential of hypervalent iodine chem., but also enriches the oxidation chem. of arylamines.

Advanced Synthesis & Catalysis published new progress about Aromatic amides Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 16426-64-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4BrNO4, Application In Synthesis of 16426-64-5.

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

Bhaumik, Asish; Eswaraiah, M. Chinna; Chakraborty, Raja published the artcile< Design and synthesis of some novel oxadiazole derivatives and evaluation of in vivo anti inflammatory activity followed by molecular docking against Cox-II enzyme>, Product Details of C7H4BrNO4, the main research area is oxadiazole mol docking anti inflammatory.

Oxadiazole is a versatile heterocyclic nucleus which attracted a wide attention of the medicinal chemists in search for new therapeutic mols. Out of its possible isomers 1, 3, 4-oxadiazole was widely exploited for various applications as medicinal agents. The literature survey revealed that 1, 3, 4-oxadiazoles were reported to possess a wide range of pharmacol. activities. The main aim and objective of the present research work was designed and synthesis of some novel 2, 5-disubstituted 1, 3, 4-oxadiazole derivatives and evaluation of in vivo anti inflammatory activity followed by mol. docking against COX II enzyme. Based on this, a new series of compounds had been planned to synthesize by reacting paraacetamidophenol, ethylchloroacetate, hydrazine monohydrate and various aromatic acids. In continuation of these research work on 2, 5-disubstituted 1, 3, 4-oxadiazole and above observation promoted to synthesize the title compounds AB1-AB8 with their potent biol. activity. Mol. docking was performed to find out the binding affinity or mol. interaction energy (kcal/mol) of docked compounds Lowest (neg. value) energy of docked mol. indicated high binding affinity with the target protein. In silico mol. docking studies, the binding energies of the synthesized compounds were found to be AB1: -4.21; AB2: -5.21; AB3: -5.06; AB4: -3.96; AB5: -4.38; AB6: -3.45; AB7: -4.25; AB8: -3.83 (k.cal/mL); standard drug diclofenac sodium: -3.15 (k.cal/mL) which indicated that the compound had high binding affinity towards the target protein cyclooxygenase with PDB id 6COX (COX II). Anti inflammatory activity of each synthesized compound was evaluated by carrageenan induced paw edema method. The activity was studied at 100 mg/kg body weight and their responses were measured at 30, 60, 120 and 180 min. The in vivo exptl. data displayed that the compound AB2, AB3, AB5 and AB7 possessed very good anti inflammatory activity among the eight synthesized compounds and all the compounds exhibited highest activity at 120 min. The percent protection (%) of the synthesized compounds were found to be AB1: 19.63 ± 0.0294, AB2: 44.19 ± 0.031**, AB3: 42.73 ± 0.0351**, AB4: 19.04 ± 0.0828ns, AB5: 39.53 ± 0.0216*, AB6: 18.91 ± 0.0310, AB7: 35.43 ± 0.0623*, AB8: 18.84 ± 0.0935ns, standard drug diclofenac sodium (DFS): 49.67 ± 0.0095** etc.

International Journal of Pharmaceutical Sciences Review and Research published new progress about Anti-inflammatory agents. 16426-64-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4BrNO4, Product Details of C7H4BrNO4.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary