6221-13-2

Usage

Uses

Used in Pharmaceutical Industry:
2-BROMO-1-PYRIDIN-4-YLETHANONE is used as a chemical intermediate for the synthesis of various drugs and pharmaceuticals. Its role in this industry is crucial as it aids in the development of new medications and the improvement of existing ones.
Used in Organic Synthesis:
In the field of organic synthesis, 2-BROMO-1-PYRIDIN-4-YLETHANONE is employed as a building block for the production of other chemical compounds. Its structural properties make it a valuable component in creating a wide range of organic molecules for various applications.

Upstream product

• 26377-17-3 ethyl 3-oxo-3-(4-pyridyl)propanoate 
• 1122-54-9 methyl (4-pyridyl) ketone 
• 1570-45-2 isonicotinic acid ethylester 

Downstream Products

• 14898-01-2 4-[2-(4,4'-dimethoxy-benzhydryl)-thiazol-4-yl]-pyridine 
• 30162-43-7 2-(3-Pyridyl)amino-4-(4-pyridyl)thiazol 
• 30235-28-0 4-pyridin-4-yl-thiazol-2-ylamine 
• 316124-45-5 1-pyridin-4-yl-2-(triphenyl-λ⁵-phiosphanylidene)ethanone 
• 118838-55-4 2-bromo-1-(pyridin-4-yl)ethanol 
• 945416-28-4 C₂₅H₃₃N₃O₂ 
• 61889-63-2 N-(4-methoxyphenyl)-4-(4-pyridinyl)-1,3-thiazol-2-amine 
• 892119-40-3 (2-methyl-5-nitro-phenyl)-(5-pyridin-4-yl-lH-imidazol-2-yl)-amine 
• 1084976-06-6 C₁₇H₁₆N₂OS₂ 
• 1084975-97-2 C₁₆H₁₄N₂OS₂ 
• 1104202-16-5 (R)-6-benzyloxymethyl-2-pyridin-4-yl-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one 
• 40353-55-7 5-pyridin-4-yl-thiazol-2-ylamine 
• 1610348-46-3 6-methyl-3-(4-nitrophenyl)-2-(pyridin-4-yl)imidazo[1,2-a]pyridine 
• 1615220-15-9 C₁₅H₁₂N₂O₂ 

Relevant academic research and scientific papers

Synthesis of 2,3-dimethylthio-6-pyridyl tetrathiafulvalene: A precursor for a new system involving a direct linkage between a strong donor (D) and a strong acceptor (A)

A multi-step synthesis of a novel tetrathiafulvalene derivative involving a 4-pyridyl substituent directly attached to the TTF moiety is described.

MULTI-STIMULI RESPONSIVE METAL-ORGANIC FRAMEWORKS

This invention relates to multi-stimuli responsive metal-organic frameworks (MOFs) comprising a repeat unit of the formula M2(L1)2(L2)2. Also disclosed are methods of preparation of multi-stimuli responsive MOFs of the formula M2(L1)2(L2)2 as well as their uses.

Design, synthesis, and biological evaluation of urea-based ROCK2 inhibitors

A series of urea-based ROCK2 inhibitors were design and synthesized. The inhibitory activity on ROCK2 was screened by enzyme-linked immunosorbent assay (ELISA). The study results showed that the urea derivatives exhibited certain ROCK2 inhibitory activity. The most potent compound 10p showed ROCK2 inhibitory activity with the IC50?value of 0.03?μM. A preliminary structure-activity relationship was then summarized. The molecular docking studies showed that further optimization needs to conduct to obtain more potent ROCK inhibitors.

SELECTIVE LIGANDS OF HUMAN CONSTITUTIVE ANDROSTANE RECEPTOR

The present invention provides a structurally novel class of heterocyclic compounds of general formula I wherein L1 is heteroaryl and L2 is heteroaryl or aryl. The novel compounds are useful in a method of prevention or treatment of a condition which is m

SUBSTITUTED PYRAZOLO[4,3-b]PYRIDINES AND THEIR USE AS GLUN2B RECEPTOR MODULATORS

Substituted pyrazolo[4,3-b]pyridines as GluN2B receptor ligands. Such compounds may be used in GluN2B receptor modulation and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by GluN2B rece

Studies on non-steroidal inhibitors of aromatase enzyme; 4-(aryl/heteroaryl)-2-(pyrimidin-2-yl)thiazole derivatives

Steroidal and non-steroidal aromatase inhibitors target the suppression of estrogen biosynthesis in the treatment of breast cancer. Researchers have increasingly focused on developing non-steroidal derivatives for their potential clinical use avoiding steroidal side-effects. Non-steroidal derivatives generally have planar aromatic structures attached to the azole ring system. One part of this ring system comprises functional groups that inhibit aromatization through the coordination of the haem group of the aromatase enzyme. Replacement of the triazole ring system and development of aromatic/cyclic structures of the side chain can increase selectivity over aromatase enzyme inhibition. In this study, 4-(aryl/heteroaryl)-2-(pyrimidin-2-yl)thiazole derivatives were synthesized and physical analyses and structural determination studies were performed. The IC50 values were determined by a fluorescence-based aromatase inhibition assay and compound 1 (4-(2-hydroxyphenyl)-2-(pyrimidine-2-yl)thiazole) were found potent inhibitor of enzyme (IC50:0.42 nM). Then, their antiproliferative activity over MCF-7 and HEK-293 cell lines was evaluated using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Compounds 1, 7, 8, 13, 15, 18, 21 were active against MCF-7 breast cancer cells. Lastly, a series of docking experiments were undertaken to analyze the crystal structure of human placental aromatase and identify the possible interactions between the most active structure and the active site.

Substituted N-Phenyl-5-(2-(phenylamino)thiazol-4-yl)isoxazole-3-carboxamides Are Valuable Antitubercular Candidates that Evade Innate Efflux Machinery

Tuberculosis remains one of the deadliest infectious diseases in the world, and the increased number of multidrug-resistant and extremely drug-resistant strains is a significant reason for concern. This makes the discovery of novel antitubercular agents a cogent priority. We have previously addressed this need by reporting a series of substituted 2-aminothiazoles capable to inhibit the growth of actively replicating, nonreplicating persistent, and resistant Mycobacterium tuberculosis strains. Clues from the structure-activity relationships lining up the antitubercular activity were exploited for the rational design of improved analogues. Two compounds, namely N-phenyl-5-(2-(p-tolylamino)thiazol-4-yl)isoxazole-3-carboxamide 7a and N-(pyridin-2-yl)-5-(2-(p-tolylamino)thiazol-4-yl)isoxazole-3-carboxamide 8a, were found to show high inhibitory activity toward susceptible M. tuberculosis strains, with an MIC90 of 0.125-0.25 μg/mL (0.33-0.66 μM) and 0.06-0.125 μg/mL (0.16-0.32 μM), respectively. Moreover, they maintained good activity also toward resistant strains, and they were selective over other bacterial species and eukaryotic cells, metabolically stable, and apparently not susceptible to the action of efflux pumps.

Synthesis method of ceftaroline fosamil intermediate 4-(4'-pyridyl)-1,3-thiazolyl-2-thiol

The invention discloses a synthesis method of an important antibiotic ceftaroline fosamil intermediate 4-(4'-pyridyl)-1,3-thiazolyl-2-thiol. The method comprises the following steps: carrying out Claisen condensation reaction on ethyl isonicotinate and ethyl acetate under alkaline conditions, carrying out acidic hydrolysis for decarboxylation, carrying out bromination reaction on the hydrolysis product and bromine, carrying out cyclization on the bromination product and ammonium dithiocarbamate, and finally, refluxing the cyclization product in glacial acetic acid to obtain the corresponding 4-(4'-pyridyl)-1,3-thiazolyl-2-thiol. The method has the advantages of fewer synthesis steps, low cost, cheap and accessible materials and low pollution, and is beneficial to industrial production.

2-mercapto-4-pyridyl thiazole synthesis method (by machine translation)

The invention discloses a synthesis method of 2-sulfydryl-4-pyridyl thiazole. According to the technical scheme, 4-acetylpyridine serving as a raw material has a bromination reaction, and then ammonium dithiocarbamate is directly added to for reaction to obtain the 2-sulfydryl-4-pyridyl thiazole. The method is simple, efficient and mild in conditions, the intermediate is a bromide, the target product can be obtained by a one-pot process without purification, and the harm of the intermediate to a human body can be greatly reduced; and moreover, the obtained product is high in purity and yield and very suitable for industrial production.

Novel arylalkenylpropargylamines as neuroprotective, potent, and selective monoamine oxidase B inhibitors for the treatment of Parkinson's disease

To develop novel neuroprotective agents, a library of novel arylalkenylpropargylamines was synthesized and tested for inhibitory activities against monoamine oxidases. From this, a number of highly potent and selective monoamine oxidase B inhibitors were identified. Selected compounds were also tested for neuroprotection in in vitro studies with PC-12 cells treated with 6-OHDA and rotenone, respectively. It was observed that some of the compounds tested yielded a marked increase in survival in PC-12 cells treated with the neurotoxins. This indicates that these propargylamines are able to confer protection against the effects of the toxins and may also be considered as novel disease-modifying anti-Parkinsonian agents, which are much needed for the therapy of Parkinson's disease.