6908-52-7

Usage

Uses

Used in Pharmaceutical Industry:
AKOS BAR-2293 is used as a pharmaceutical intermediate for the synthesis of various pharmaceutical compounds. Its unique chemical structure and properties make it a valuable building block in the development of new drugs and medications.
Used in Organic Synthesis:
AKOS BAR-2293 is used as an organic building block in the synthesis of other compounds. Its versatile chemical structure allows it to be incorporated into a wide range of organic molecules, contributing to the development of new chemical entities and materials.
It is important to handle and store AKOS BAR-2293 according to appropriate safety and handling guidelines to prevent any potential hazards.

Upstream product

• 5720-05-8 4-methylphenylboronic acid 
• 1878-68-8 2-(4-bromophenyl)-acetic acid 
• 106-38-7 para-bromotoluene 
• 15738-23-5 sodium tetrakis(4-tolyl)borate 
• 124-38-9 carbon dioxide 
• 37859-24-8 2-(4-bromophenyl)acetyl chloride 

Relevant academic research and scientific papers

THIAZOLOPIPERAZINE DERIVATIVES AND COMPOSITION FOR PREVENTING OR TREATING AUTOIMMUNE DISEASES COMPRISING THE SAME

The present invention provides a thiazolopiperazine derivative, and a pharmaceutical composition and a health functional food composition for preventing or treating autoimmune diseases containing the same as an active component. A compound represented by chemical formula 1 or a pharmaceutically acceptable salt thereof according to the present invention can have an effect of inhibiting lysophosphatidic acid 1 (LPA1) receptor activation, thereby being able to be usefully used as the pharmaceutical composition or the health functional food composition for preventing or treating LPA1-related diseases. In addition, it is possible to effectively prevent or treat not only autoimmune diseases, but also other immune-related diseases with similar mechanisms of occurrence by using the pharmaceutical composition and the health functional food composition.COPYRIGHT KIPO 2020

Green synthesis of biphenyl carboxylic acids via Suzuki–Miyaura cross-coupling catalyzed by a water-soluble fullerene-supported PdCl2 nanocatalyst

A green synthesis of variously substituted biphenyl carboxylic acids was achieved through Suzuki–Miyaura cross-coupling of a bromobenzoic acid with an aryl boronic acid using a water-soluble fullerene-supported PdCl2 nanocatalyst (C60-TEGs/ PdCl2). Yields of more than 90% were obtained at room temperature in 4 h using 0.05 mol% catalyst and 2 equiv. K2CO3.

Visible-Light-Driven External-Reductant-Free Cross-Electrophile Couplings of Tetraalkyl Ammonium Salts

Cross-electrophile couplings between two electrophiles are powerful and economic methods to generate C-C bonds in the presence of stoichiometric external reductants. Herein, we report a novel strategy to realize the first external-reductant-free cross-electrophile coupling via visible-light photoredox catalysis. A variety of tetraalkyl ammonium salts, bearing primary, secondary, and tertiary C-N bonds, undergo selective couplings with aldehydes/ketone and CO2. Notably, the in situ generated byproduct, trimethylamine, is efficiently utilized as the electron donor. Moreover, this protocol exhibits mild reaction conditions, low catalyst loading, broad substrate scope, good functional group tolerance, and facile scalability. Mechanistic studies indicate that benzyl radicals and anions might be generated as the key intermediates via photocatalysis, providing a new direction for cross-electrophile couplings.

Method for synthesizing biphenylcarboxylic acid compound by using Suzuki coupling reaction

The invention provides a method for synthesizing a biphenylcarboxylic acid compound by using the Suzuki coupling reaction. According to the method, brominated aromatic hydrocarbon and arylboronic acidare used as raw materials, and water-soluble fullerene nanopalladium is used as a catalyst; and the equation of the Suzuki coupling reaction is as described in the specification. In the equation, R1and R2 represent substituents at different positions, may be acceptor or donor substituents, and may be monosubstitutents or polysubstitutent; and R1 and R2 may be identical or different groups. The water-soluble fullerene nanopalladium catalyst is cheap, easily available and environmentally friendly, and has high catalytic activity and stable properties. When the catalyst is used for catalysis ofthe Suzuki coupling reaction, conditions are mild, anhydrous anaerobic treatment and high-temperature treatment are not needed, and cost is low. The method can be applied to the industrial synthesisof non-steroidal anti-inflammatory drugs such as diphenylacetic acid and diflunisal.

1, 3, 5 - cyclohexanetriol - cis - or organic boronic acid-stable siloxy inositol complex and organic synthetic reaction using a reagent art

PROBLEM TO BE SOLVED: To provide a stable ate-type complex of an organoboronic acid as a reagent for organic synthesis reaction; and manufacturing techniques thereof.SOLUTION: A stable ate-type complex of an organoboronic acid with scyllo-inositol or 1,3,5-cis-cyclohexanetriol comprises an anion represented by the specified general formula (I) or (II) as a constituent. In the formula, Rand Reach represent an alkyl group, alkenyl group, alkynyl group, aryl group, heterocyclic group or aralkyl group which may have substituents.

A highly efficient catalyst of a nitrogen-based ligand for the Suzuki coupling reaction at room temperature under air in neat water

Glycine, as a kind of commercially available and inexpensive ligand, is used to prepare an air-stable and water-soluble catalyst for the Suzuki-Miyaura reaction in our study. In the presence of 0.1% [PdCl2(NH 2CH2COOH)2] as the catalyst, extremely excellent catalytic activity towards the Suzuki-Miyaura coupling of aryl halides containing the carboxyl group with various aryl boronic acids is observed at room temperature under air in neat water. the Partner Organisations 2014.

Palladium charcoal-catalyzed, ligandless Suzuki reaction by using tetraarylborates in water

In water and without using any ligand, palladium charcoal-catalyzed Suzuki coupling reaction of tetraarylborates with aryl bromides could be achieved in excellent yield. A concise mechanism consisting of four catalytic cycles is depicted in this paper.

Functionalized carbosilane dendritic species as soluble supports in organic synthesis

A new methodology, which is compatible with the use of reactive organometallic reagents, has been developed for the use of carbosilane dendrimers as soluble supports in organic synthesis. Hydroxy-functionalized dendritic carbosilanes Si[CH2CH2CH2SiMe2(C6H4CH(R)OH)]4 (G0-OH, R = H or (S)-Me) and Si[CH2CH2CH2Si[CH2CH2CH2SiMe2(C6H4CH(R)OH)]3]4 (G1-OH, R = H or (S)-Me) were prepared and subsequently converted into the esters Si[CH2CH2CH2SiMe2(C6H4-CH(R)OC(O)CH2Ph)]4 (R = H or (S)-Me) and Si[CH2CH2CH2Si[CH2CH2CH2SiMe2(C6H4CH(R)OC-(O)CH2C6H4R')]3]4 (R = H and R' = H or R = (S)-Me and R' = H or R = H and R' = Br). As an example the latter compound was functionalized under Suzuki conditions. The functionalized carboxylic acid was obtained in high yield after cleavage from the dendritic support. Moreover, the ester functionalized dendrimers were converted to the corresponding zinc enolates followed by a condensation reaction with an imine to a β-lactam in excellent yield and purity. Furthermore, it was demonstrated that a small combinatorial library of β-lactams could be prepared starting from a carbosilane dendrimer functionalized with different ester moieties. These results show that carbosilane dendrimers can be applied as soluble substrate carriers for the generation of low molecular weight organic molecules. In combination with nanofiltration techniques, separation and recycling of the dendrimers can be realized.

Photostimulated reactions of phenylacetic acid dianions with aryl halides. Influence of the metallic cation on the regiochemistry of arylation.

[reaction: see text]Phenylacetic acid dianions react via what appears to be an S(RN)1 process with aryl halides under photostimulation to afford aryl substitution products 5 and 6. When the counterion is K+, only 4-biphenylacetic acids 5 are obtained. Both alpha- and para-coupling occurs with Na+ to give a mixture of 5 and 6, while exclusive formation of diphenylacetic acids 6 is observed with the dilithio salt of 1.

Palladium-catalyzed alkylatiqns in aqueous media

The efficient, catalytic alkylation of biomolecules and other organic substrates in aqueous media has been demonstrated. The water-soluble Pd(0) complex Pd(PPh2(m-C6H4SO3M))3 (2: M = Na+, K+) was isolated and characterized by single-crystal X-ray diffraction. The relevant crystal data for this complex are as follows (M = K+): a = 12.618 (1) ?, b = 19.532 (2) ?, c = 24.423 (3) ?, α = 100.65 (1)°, β= 94.37 (1)°, γ = 99.10 (1)°; P1?, T = -70 °C, dc = 1.514 g/cm3, μ = 7.74 cm-1, 14423 reflections; R = 0.054, Rw = 0.053. Crystalline, air-sensitive 2 catalyzed alkylation reactions in a variety of single-phase aqueous solvent systems. Hydrophobic or hydrophilic aryl and heteroaromatic halides underwent coupling reactions with aryl or vinyl boronic acids, alkynes, an alkene, and a dialkyl phosphite. Examples of the alkylation of biomolecules in aqueous media included the coupling of alkynes with unprotected iodonucleotides, iodonucleoside, and an iodoamino acid. This approach provided an alternative, convergent synthesis of T-505, part of a family of chain-terminating nucleotide reagents used in DNA sequencing and labeling.