456-00-8

Usage

Uses

Used in Pharmaceutical Synthesis:
2-AMINO-4'-FLUOROACETOPHENONE HYDROCHLORIDE is used as a reagent in the synthesis of various pharmaceuticals and organic compounds due to its unique chemical structure and properties.
Used in Medicinal Chemistry Research:
In the field of medicinal chemistry, 2-AMINO-4'-FLUOROACETOPHENONE HYDROCHLORIDE is used as a research tool to study its potential applications in drug development, particularly for its antibacterial, antifungal, and anti-inflammatory properties.
Used in Drug Development:
2-AMINO-4'-FLUOROACETOPHENONE HYDROCHLORIDE is utilized in drug development for its potential therapeutic effects, including its ability to combat bacterial and fungal infections and reduce inflammation, making it a promising candidate for the creation of new medications.

Upstream product

• 89204-90-0 5-(4-Fluoro-phenyl)-oxazole-4-carboxylic acid methyl ester 
• 7468-87-3 (4-fluoro-phenacyl)-hexamethylenetetraminium; bromide 
• 456-04-2 2-Chloro-4'-fluoroacetophenone 
• 403-29-2 2-bromo-4'-fluoroacetophenone 
• 82585-50-0 2-[2-(4-fluoro-phenyl)-2-oxo-ethyl]-isoindole-1,3-dione 
• 369-43-7 2-amino-1-(4-fluorophenyl)ethan-1-one 
• 118887-70-0 2-azido-1-(4-fluoro-phenyl)-ethanone 
• 403-42-9 1-(4-fluorophenyl)ethanone 
• 875306-84-6 C₁₀H₈FNO₃ 

Downstream Products

• 99923-42-9 Thiophene-3-carboxylic acid [2-(4-fluoro-phenyl)-2-oxo-ethyl]-amide 
• 115859-12-6 5-(4-fluorophenyl)-2,3-dihydroimidazo<2,1-b>thiazole 
• 17452-29-8 1-methyl-5-(4-fluorophenyl)imidazole-2-thione 
• 64748-82-9 2-(2,4-dioxo-imidazolidin-1-ylimino)-N-[2-(4-fluoro-phenyl)-2-oxo-ethyl]-acetamide 
• 864535-60-4 1-(4-chloro-phenyl)-5-(4-fluoro-phenyl)-1H-imidazole-2-thiol 
• 456-05-3 2-amino-1-(4-fluorophenyl)ethanol 
• 864535-60-4 C₁₅H₁₀ClFN₂S 
• 704915-90-2 3-amino-2-(4-fluoro-phenyl)-quinoline-4-carboxylic acid 

Relevant academic research and scientific papers

The reaction of prop-2-ynylsulfonium salts and sulfonyl-protected β-amino ketones to epoxide-fused 2-methylenepyrrolidines and S-containing pyrroles

A novel divergent domino annulation reaction of prop-2-ynylsulfonium salts with sulfonyl-protected β-amino ketones has been developed, affording various epoxide-fused 2-methylenepyrrolidines and S-containing pyrroles in moderate to excellent yields. Prop-2-ynylsulfonium salts act as C2synthons in the reactions providing a promising epoxide-fused skeleton in a single operation with readily accessible starting materials.

Synthesis, characterization, COX1/2 inhibition and molecular modeling studies on novel 2-thio-diarylimidazoles

Heterocyclic compounds with diaryl substituents have been a milestone approach for selective cyclooxygenase 2 (COX 2) inhibition by bioisosteric replacements and modifications. It is also known that thiazole derivatives have different pharmacological acti

Structural Basis for EGFR Mutant Inhibition by Trisubstituted Imidazole Inhibitors

Acquired drug resistance in epidermal growth factor receptor (EGFR) mutant non-small-cell lung cancer is a persistent challenge in cancer therapy. Previous studies of trisubstituted imidazole inhibitors led to the serendipitous discovery of inhibitors that target the drug resistant EGFR(L858R/T790M/C797S) mutant with nanomolar potencies in a reversible binding mechanism. To dissect the molecular basis for their activity, we determined the binding modes of several trisubstituted imidazole inhibitors in complex with the EGFR kinase domain with X-ray crystallography. These structures reveal that the imidazole core acts as an H-bond acceptor for the catalytic lysine (K745) in the "αC-helix out" inactive state. Selective N-methylation of the H-bond accepting nitrogen ablates inhibitor potency, confirming the role of the K745 H-bond in potent, noncovalent inhibition of the C797S variant. Insights from these studies offer new strategies for developing next generation inhibitors targeting EGFR in non-small-cell lung cancer.

Design, synthesis and biological evaluation of new Axl kinase inhibitors containing 1,3,4-oxadiazole acetamide moiety as novel linker

Using the principle of bioisosteric replacement, we present a structure-based design approach to obtain new Axl kinase inhibitors with significant activity at the kinase and cellular levels. Through a stepwise structure-activity relationships exploration, a series of 6,7-disubstituted quinoline derivatives, which contain 1,3,4-oxadiazol acetamide moiety as novel Linker, were ultimately synthesized with Axl as the primary target. Most of them exhibited moderate to excellent activity, with IC50 values ranging from 0.032 to 1.54 μM against the tested cell lines. Among them, the most promising compound 47e, as an Axl kinase inhibitor (IC50 = 10 nM), shows remarkable cytotoxicity against A549, HT-29, PC-3, MCF-7, H1975 and MDA-MB-231 cell lines. More importantly, 47e also shows a significant inhibitory effect on EGFR-TKI resistant NSCLC cell lines H1975/gefitinib. Meanwhile, this study provides a novel type of linker for Axl kinase inhibitors, namely 1,3,4-oxadiazol acetamide moiety, which is out of the scope of the “5- atoms role ".

Combating fluconazole-resistant fungi with novel β-azole-phenylacetone derivatives

A series of β-azole-phenylacetone derivatives with novel structures were designed and synthesized to combat the increasing incidence of susceptible fungal infections and drug-resistant fungal infections. The antifungal activity of the synthesized compounds was assessed against five susceptible strains and five fluconazole-resistant strains. Antifungal activity tests showed that most of the compounds exhibited excellent antifungal activities against five pathogenic strains with MIC values in the range of 0.03–1 μg/mL. Compounds with R1 = 3-F substituted and 15o and 15ae exhibited moderate antifungal activities against fluconazole-resistant strains 17# and CaR with MIC values in the range of 1–8 μg/mL. Compounds with R1 = H or 2-F (such as 15a, 15o, 15p) displayed moderate to good antifungal activity against fluconazole-resistant strains 632, 901 and 904 with MIC values in the range of 0.125–4 μg/mL. Notably, 15o and 15ae exhibited antifungal activity against five susceptible strains and five fluconazole-resistant strains. Preliminary mechanistic studies showed that the potent antifungal activity of compound 15ae stemmed from inhibition of C. albicans CYP51. Compounds 15o, 15z and 15ae were nearly nontoxic to mammalian A549 cells.

DOPAMINE D3 RECEPTOR ANTAGONISTS HAVING A MORPHOLINE MOIETY

The disclosure provides compounds of formula (I) or pharmaceutically acceptable salts thereof: The disclosure also provides processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them, and their use

CYCLOPROPYL DERIVATIVES AS ROR-GAMMA MODULATORS

The present invention provides compounds which are modulators of RORγ and their use for the treatment of diseases or conditions mediated by RORγ. Further, the present invention relates to processes of preparing such compounds, their tautomeric forms, novel intermediates involved in their synthesis, their pharmaceutically acceptable salts, methods for using such compounds and pharmaceutical compositions containing them (Formula I).

3,4-diaryl maleimide derivative and preparation method and application thereof

The invention discloses a 3,4-diaryl maleimide derivative represented by a general formula I and a medicinal salt form thereof. The invention further discloses a preparation method of the mentioned 3,4-diaryl maleimide derivative and application of the 3,

3. 4 - diaryl maleic imide derivative and its preparation method and application

The invention discloses a 3,4-diarylmaleimide derivative and a preparation method as well as application thereof. The general formula of the 3,4-diarylmaleimide derivative is shown in the specification. The 3,4-diarylmaleimide derivative can be applied to

Discovery of 2-azetidinone and 1H-pyrrole-2,5-dione derivatives containing sulfonamide group at the side chain as potential cholesterol absorption inhibitors

Cholesterol absorption inhibitor (CAI) targeting Niemann-Pick C1-like1 protein was developed for the treatment of hyperlipidaemia and only ezetimibe was approved so far. For developing novel CAIs, we synthesized sixteen 2-azetidinone derivatives and thirt