216768-18-2

Upstream product

• 5446-02-6 4-methoxymethylsalicylate 
• 107-83-5 2-Methylpentane 
• 358-23-6 trifluoromethylsulfonic anhydride 
• 2237-36-7 4-methoxysalicylic acid 

Downstream Products

• 910240-95-8 methyl 2-(4-fluoroanilino)-4-methoxybenzoate 
• 872550-16-8 methyl 2-(cyclopropylethynyl)-4-(methyloxy)benzoate 
• 86611-38-3 4-methoxy-2-(4-carboxyphenylamino)benzoic acid 
• 1359967-23-9 4-methoxy-2-(3,5-bis(methoxy)phenylamino)benzoic acid 
• 1359967-81-9 4-methoxy-2-(3,5-bis(methoxy)phenylamino)benzoic acid methyl ester 
• 1359967-14-8 4-methoxy-2-(3-nitrophenylamino)benzoic acid 
• 1359967-68-2 4-methoxy-2-(3-nitrophenylamino)benzoic acid methyl ester 
• 1359967-16-0 4-methoxy-2-(3-methylphenylamino)benzoic acid 
• 1359967-71-7 4-methoxy-2-(3-methylphenylamino)benzoic acid methyl ester 
• 857599-82-7 4-methoxy-2-(3-chlorophenylamino)benzoic acid 
• 1359967-69-3 4-methoxy-2-(3-chlorophenylamino)benzoic acid methyl ester 
• 19218-83-8 5-methoxydiphenylamine-2-carboxylic acid 
• 1359967-18-2 4-methoxy-2-(4-nitrophenylamino)benzoic acid 
• 1359967-73-9 4-methoxy-2-(4-nitrophenylamino)benzoic acid methyl ester 

Relevant academic research and scientific papers

Organic electroluminescent element

By manufacturing an organic EL element using a material for a light emitting layer including a pyrene-based compound represented by the following formula (2) as a host material and a polycyclic aromatic compound in which a plurality of aromatic rings is linked with a boron atom and a nitrogen atom or an oxygen atom as a dopant material, an organic EL element having, for example, excellent light emission efficiency is provided. In the above formula (2), at least one hydrogen atom in a pyrene moiety may be substituted by an aryl having 6 to 10 carbon atoms or the like. Ar represents an aryl having 14 to 40 carbon atoms or a heteroaryl having 12 to 40 carbon atoms. These groups may be substituted by an aryl having 6 to 10 carbon atoms or the like. s and p each independently represent an integer of 1 or 2. s and p do not simultaneously represent 2. One or more hydrogen atoms in a compound represented by formula (2) may be each independently substituted by a halogen atom, cyano, or a deuterium atom.

Lead Optimization of Second-Generation Acridones as Broad-Spectrum Antimalarials

The global impact of malaria remains staggering despite extensive efforts to eradicate the disease. With increasing drug resistance and the absence of a clinically available vaccine, there is an urgent need for novel, affordable, and safe drugs for prevention and treatment of malaria. Previously, we described a novel antimalarial acridone chemotype that is potent against both blood-stage and liver-stage malaria parasites. Here, we describe an optimization process that has produced a second-generation acridone series with significant improvements in efficacy, metabolic stability, pharmacokinetics, and safety profiles. These findings highlight the therapeutic potential of dual-stage targeting acridones as novel drug candidates for further preclinical development.

ORGANIC ELECTROLUMINESCENT ELEMENT

Provided is an organic electroluminescent element including a light emitting layer containing, as a dopant, at least two compounds selected from a compound group consisting of a polycyclic aromatic compound represented by the following general formula (1) and a multimer thereof: wherein the symbols are defined in the specification.

Discovery and Structural Optimization of Acridones as Broad-Spectrum Antimalarials

Malaria remains one of the deadliest diseases in the world today. Novel chemoprophylactic and chemotherapeutic antimalarials are needed to support the renewed eradication agenda. We have discovered a novel antimalarial acridone chemotype with dual-stage activity against both liver-stage and blood-stage malaria. Several lead compounds generated from structural optimization of a large library of novel acridones exhibit efficacy in the following systems: (1) picomolar inhibition of in vitro Plasmodium falciparum blood-stage growth against multidrug-resistant parasites; (2) curative efficacy after oral administration in an erythrocytic Plasmodium yoelii murine malaria model; (3) prevention of in vitro Plasmodium berghei sporozoite-induced development in human hepatocytes; and (4) protection of in vivo P. berghei sporozoite-induced infection in mice. This study offers the first account of liver-stage antimalarial activity in an acridone chemotype. Details of the design, chemistry, structure-activity relationships, safety, metabolic/pharmacokinetic studies, and mechanistic investigation are presented herein.

Concise Synthesis of a Potential 5-Lipoxygenase Activating Protein (FLAP) Inhibitor and Its Analogs through Late-Stage Alkene Dicarbofunctionalization

We report a five-step synthesis of the biologically important 1,1-diarylalkane 1, a potential 5-lipoxygenase activating protein (FLAP) inhibitor that was synthesized previously in 12 steps. In this synthesis, we apply a three-component alkene dicarbofunct

ORGANIC ELECTROLUMINESCENT ELEMENT

An organic electroluminescent element includes a light emitting layer including, as host materials, an anthracene-based compound represented by the following general formula (1) and a dibenzochrysene-based compound represented by the following general for

ORGANIC ELECTROLUMINESCENT ELEMENT

Provided is an organic electroluminescent element having optimal light emission characteristics. The above problem is solved by an organic electroluminescent element having a light emitting layer containing a compound of formula (1) or a multimer compound having a plurality of structures of formula (1), and a compound of formula (2A) or (2B) in formula (1), ring A, ring B, and ring C each represent an aryl ring or the like, X1 and X2 each represent >O or >N—R, and the R represents an aryl or the like, and in formula (2A) or (2B), X represents an aryl or the like, and Z represents a single bond, a divalent group, or the like.

BORONIC ACID OR BORONIC ESTER, OR METHOD OF PRODUCING POLYCYCLIC AROMATIC COMPOUND OR POLYCYCLIC AROMATIC POLYMER COMPOUND USING THEM

PROBLEM TO BE SOLVED: To provide a boronic acid compound effective in producing a polycyclic aromatic compound, and a method of producing a polycyclic aromatic compound using the boronic acid compound. SOLUTION: A polycyclic aromatic compound is produced by causing an acid to act on a compound represented by the general formula (1) in the figure. In the formula, the A ring, B ring and C ring are each independently an aryl ring or heteroaryl ring; Y1 is optionally esterified -B(OH)2; and X1 and X2 are -O-, >N-Ar (Ar is aryl or the like), -S-, or -Se-. COPYRIGHT: (C)2018,JPOandINPIT

Compound and organic light emitting device comprising same

Disclosed are a compound represented by chemical formula 1 and an organic light emitting device comprising the same. Descriptions about substituent groups in chemical formula 1 refer to the detailed description of the present invention.COPYRIGHT KIPO

Synthesis and antimicrobial evaluation of amixicile-based inhibitors of the pyruvate-ferredoxin oxidoreductases of anaerobic bacteria and Epsilonproteobacte

Amixicile is a promising derivative of nitazoxanide (an antiparasitic therapeutic) developed to treat systemic infections caused by anaerobic bacteria, anaerobic parasites, and members of the Epsilonproteobacteria (Campylobacter and Helicobacter). Amixicile selectively inhibits pyruvate-ferredoxin oxidoreductase (PFOR) and related enzymes by inhibiting the function of the vitamin B1 cofactor (thiamine pyrophosphate) by a novel mechanism. Here, we interrogate the amixicile scaffold, guided by docking simulations, direct PFOR inhibition assays, and MIC tests against Clostridium difficile, Campylobacter jejuni, and Helicobacter pylori. Docking simulations revealed that the nitro group present in nitazoxanide interacts with the protonated N4′-aminopyrimidine of thiamine pyrophosphate (TPP). The ortho-propylamine on the benzene ring formed an electrostatic interaction with an aspartic acid moiety (B456) of PFOR that correlated with improved PFOR-inhibitory activity and potency by MIC tests. Aryl substitution with electron-withdrawing groups and substitutions of the propylamine with other alkyl amines or nitrogen-containing heterocycles both improved PFOR inhibition and, in many cases, biological activity against C. difficile. Docking simulation results correlate well with mechanistic enzymology and nuclear magnetic resonance (NMR) studies that show members of this class of antimicrobials to be specific inhibitors of vitamin B1 function by proton abstraction, which is both novel and likely to limit mutation-based drug resistance.