87700-60-5

Upstream product

• 5773-80-8 6-bromo-2-naphthoic acid 
• 79-37-8 oxalyl dichloride 
• 4732-69-8 Chloro-oxo-acetic acid 

Downstream Products

• 87700-75-2 6-bromo-N-phenyl-2-naphthamide 
• 870822-84-7 2-bromo-6-chloronaphthalene 
• 935472-87-0 2-(6-bromonaphthalen-2-yl)-1-phenyl-1H-benzimidazole 
• 1135540-71-4 (R)-2-(2-fluoropropyl)phenyl 6-bromo-2-naphthoate 
• 1255871-55-6 6-bromonaphthalene-2-carboxamide 
• 426219-18-3 orteronel 
• 1346155-54-1 N,N-diisopropyl-6-[1-hydroxy-1-(1-trityl-1H-imidazol-4-yl)methyl]-2-naphthamide 
• 426219-47-8 N,N-diisopropyl-6-[(1-trityl-1H-imidazol-4-yl)carbonyl]-2-naphthamide 
• 566939-85-3 Orteronel 
• 752243-39-3 6-(7-hydroxy-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-7-yl)-N-methylnaphthalene-2-carboxamide 
• 426219-58-1 tert-butyl (S)-3-(6-(diisopropylcarbamoyl)naphthalen-2-yl)-3-hydroxy-3-(1-trityl-1H-imidazol-4-yl)propanoate 
• 426219-53-6 2C₁₀H₁₁NO₅*C₁₈H₁₇N₃O₂ 
• 50637-83-7 2-bromo-1-(6-bromonaphthalen-2-yl)ethanone 
• 1256387-44-6 1-(6-bromo-naphthalen-2-yl)-2-diazo-ethanone 

Relevant academic research and scientific papers

Metallogels self-assembled from linear rod-like platinum complexes: Influence of the linkage

Two linear rod-like platinum complexes, which only differed in the linkage, were prepared. They both self-assemble into metallogels in nonpolar solvents; however, a very big contrast was observed. Unexpectedly, a much weaker gel was acquired upon replacing the ester linkage by an amide group. The intermolecular hydrogen bonding offered by the amide motif leads to a different stacking fashion and mechanism. The results demonstrated herein contribute to the rational design of metallogels as well as other functional supramolecular materials.

Cobalt-Catalyzed Radical Hydroamination of Alkenes with N-Fluorobenzenesulfonimides

An efficient and general radical hydroamination of alkenes using Co(salen) as catalyst, N-fluorobenzenesulfonimide (NFSI) and its analogues as both nitrogen source and oxidant was successfully disclosed. A variety of alkenes, including aliphatic alkenes, styrenes, α, β-unsaturated esters, amides, acids, as well as enones, were all compatible to provide desired amination products. Mechanistic experiments suggest that the reaction underwent a metal-hydride-mediated hydrogen atom transfer (HAT) with alkene, followed by a pivotal catalyst controlled SN2-like pathway between in situ generated organocobalt(IV) species and nitrogen-based nucleophiles. Moreover, by virtue of modified chiral cobalt(II)-salen catalyst, an unprecedented asymmetric version was also achieved with good to excellent level of enantiocontrol. This novel asymmetric radical C?N bond construction opens a new door for the challenging asymmetric radical hydrofunctionalization.

Discovery of methoxy-naphthyl linked N-(1-benzylpiperidine) benzamide as a blood-brain permeable dual inhibitor of acetylcholinesterase and butyrylcholinesterase

The cholinesterase enzymes play a vital role in maintaining balanced levels of the neurotransmitter acetylcholine in the central nervous system. However, the overexpression of these enzymes results in hampered neurotransmission. Both the major forms of cholinesterase enzymes viz. acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) play a crucial role in blocking neurotransmission; therefore, in recent years, a strategy of dual cholinesterase inhibition is being explored. Herein, we developed an energy-optimized e-pharmacophore hypothesis AHHPRR from AChE-donepezil complex and screened a set of 15 scaffolds that were designed imaginarily. The ligand with N-(1-benzylpyridinium) benzamide framework has shown the highest fitness and volume score, which was chosen for synthesis and validation. A series of pyridinium benzamides were synthesized and screened for cholinesterase inhibition that led to the identification of 7b, a naphthalene containing N-(1-benzylpiperidine) benzamide as a potent dual AChE and BChE inhibitor with IC50 values of 0.176, and 0.47 μM, respectively. The kinetic study indicated that 7b inhibits AChE in a non-competitive manner with Ki value of 0.21 μM, and BChE in a mixed-fashion with Ki of 0.15 μM. The observed mode of inhibition was corroborated with molecular docking studies. The MD simulation studies pointed out that both AChE and BChE undergo low conformational changes in complex with 7b. The benzamide 7b displayed high BBB permeability in PAMPA assay, which indicates its potential for further exploration in preclinical studies for Alzheimer's disease.

COMPOSITION AND METHOD FOR MANUFACTURING DEVICE USING SAME

An onium salt and a composition having high sensitivity and excellent pattern characteristics such as LWR, which is preferably used for a resist composition for a lithography process using two active energy rays of a first active energy ray such as an electron beam or an extreme ultraviolet and a second active energy ray such as UV.

Benzimidazole compound and derivatives, organic electronic transmission material as well as preparation of benzimidazole compound and derivatives and application of organic electronic transmission material

The invention belongs to the technical field of an organic photoelectric functional molecular material and discloses a benzimidazole compound and derivatives, an organic electronic transmission material as well as preparation of the benzimidazole compound and derivatives and application of the organic electronic transmission material. The organic electronic transmission material comprises at leastone of benzimidazole compound derivatives. The structure of the benzimidazole compound derivatives is as shown in a formula II or a formula III. The method comprises the following steps: (a) in a catalytic system, performing Suzuki reaction of the benzimidazole compound and double pinacol diborane and performing subsequent treatment to obtain a product containing boric acid ester; (b) in the catalytic system, performing coupling reaction of the product containing boric acid ester and 3-bromine-1,10-phenanthroline or 2-chlorine-4,6-diphenyl-1,3,5-triazine and performing subsequent treatment toobtain the benzimidazole compound derivatives. The organic electronic transmission material has high heat stability and film appearance stability and is favorable for improving the stability of devices; and the synthesis method is simple and easy in purification. (The formula is as shown in the description).

Identification and Structure-Activity Relationships of Novel Compounds that Potentiate the Activities of Antibiotics in Escherichia coli

In Gram-negative bacteria, efflux pumps are able to prevent effective cellular concentrations from being achieved for a number of antibiotics. Small molecule adjuvants that act as efflux pump inhibitors (EPIs) have the potential to reinvigorate existing antibiotics that are currently ineffective due to efflux mechanisms. Through a combination of rigorous experimental screening and in silico virtual screening, we recently identified novel classes of EPIs that interact with the membrane fusion protein AcrA, a critical component of the AcrAB-TolC efflux pump in Escherichia coli. Herein, we present initial optimization efforts and structure-activity relationships around one of those previously described hits, NSC 60339 (1). From these efforts we identified two compounds, SLUPP-225 (17h) and SLUPP-417 (17o), which demonstrate favorable properties as potential EPIs in E. coli cells including the ability to penetrate the outer membrane, improved inhibition of efflux relative to 1, and potentiation of the activity of novobiocin and erythromycin.

N - heterocyclic compound, intermediate, preparation method, pharmaceutical composition and application (by machine translation)

The invention discloses a N - heterocyclic compound, intermediate, preparation method, pharmaceutical composition and application. The invention of SHP2 N - heterocyclic compound to have high selectivity, can effectively inhibit the cell in the SHP2 downstream signal path ERK phosphorylation level, to tumor cells has very good inhibition activity, it has broad drug development prospects; its preparation method is simple, mild reaction conditions, high yield and purity, after treatment is simple, environmental protection, and is favorable for industrial production. (by machine translation)

NEW NITROGEN-CONTAINING HETEROCYCLIC COMPOUNDS AND ORGANIC ELECTRONIC DEVICE USING THE SAME

The present invention refers to novel nitrogenous heterocyclic and optical material using it organic electronic device with high. The present invention according to organic electronic devices efficiency, excellent characteristics such as voltage and life blades, presenting a. (by machine translation)

Discovery of ledipasvir (GS-5885): A potent, once-daily oral NS5A inhibitor for the treatment of hepatitis C virus infection

A new class of highly potent NS5A inhibitors with an unsymmetric benzimidazole-difluorofluorene-imidazole core and distal [2.2.1]azabicyclic ring system was discovered. Optimization of antiviral potency and pharmacokinetics led to the identification of 39 (ledipasvir, GS-5885). Compound 39 (GT1a replicon EC50 = 31 pM) has an extended plasma half-life of 37-45 h in healthy volunteers and produces a rapid >3 log viral load reduction in monotherapy at oral doses of 3 mg or greater with once-daily dosing in genotype 1a HCV-infected patients. 39 has been shown to be safe and efficacious, with SVR12 rates up to 100% when used in combination with direct-acting antivirals having complementary mechanisms.

Naphthalenyl derivatives for hitting P-gp/MRP1/BCRP transporters

Substituted naphthalenyl derivatives bearing oxazole, or thiazole or furyl heteronuclei have been carried out as bioisosters of aryl-oxazoles and -thiazoles derivatives previously reported in order to investigate the role of the hindrance on the activity towards P-gp/BCRP/and MRP1 transporters. In addition, the role of naphthalenyl group to modulate P-gp intrinsic activity of these compounds was ascertained. The results demonstrated that all naphthalenyl derivatives displayed comparable P-gp activity with respect to lead compounds previously characterized in our SAR studies but were less active towards BCRP and MRP1 pumps. In terms of intrinsic activity, the replacement of aryl with naphthalenyl moiety led to P-gp inhibitors, unambiguous or ambiguous substrates on the base of the heteronucleus and the substituent on the naphthalenyl fragment. Indeed, oxazole derivatives were: inhibitors (R = H, F, OH), unambiguous substrates (R = OCH3), or ambiguous substrate (R = Br); thiazole derivatives were: unambiguous substrates (R = OCH3, Br), or ambiguous substrates (R = H, F). Finally furyl derivatives were ambiguous substrates.