95262-10-5

Usage

Uses

Used in Pharmaceutical Industry:
3-(4-fluorophenylamino)-3-oxopropanoic acid is used as a key intermediate for the synthesis of various pharmaceutical drugs. Its unique structure allows for the development of new medications with potential therapeutic benefits.
Used in Medicinal Chemistry:
In the field of medicinal chemistry, 3-(4-fluorophenylamino)-3-oxopropanoic acid is utilized as a starting material for the design and synthesis of novel compounds with potential medicinal properties. Its incorporation into drug candidates can lead to the discovery of new treatments for various diseases.
Used in Drug Design:
3-(4-fluorophenylamino)-3-oxopropanoic acid plays a crucial role in drug design, where it can be modified and combined with other chemical entities to create innovative pharmaceutical agents. Its adaptability makes it a valuable component in the development of new drugs with improved efficacy and safety profiles.

Upstream product

• 130112-64-0 methyl 3-(4-fluorophenylamino)-3-oxopropanoate 
• 141-82-2 malonic acid 
• 371-40-4 4-fluoroaniline 
• 2033-24-1 cycl-isopropylidene malonate 
• 104330-60-1 3-((4-fluorophenyl)amino)-3-oxo-propionic acid ethyl ester 

Downstream Products

• 888717-80-4 C₂₂H₁₆F₂N₄O₃ 
• 1474049-68-7 (Z)-N¹-(3-((1H-pyrrol-2-yl)methylene)-2-oxoindolin-6-yl)-N³-(4-fluorophenyl)malonamide 
• 1474049-67-6 N¹-(4-fluorophenyl)-N³-(2-oxoindolin-6-yl)malonamide 
• 849217-68-1 cabozantinib 
• 1677-37-8 6-fluoro-4-hydroxy-1H-quinolin-2-one 
• 888854-89-5 C₂₉H₃₁F₂N₇O₄ 
• 888720-43-2 C₂₆H₂₆F₂N₆O₄ 
• 888854-84-0 C₂₇H₂₈F₂N₆O₄ 
• 888854-85-1 C₂₈H₂₈F₂N₆O₅ 
• 864440-16-4 N-(4-Fluorophenyl)-N'-(4-{2-[(morpholine-4-carbonyl)amino]pyridin-4-yloxy}phenyl)malonamide 
• 864241-93-0 N-{4-[2-(3,3-Dimethylureido)pyridin-4-yloxy]phenyl}-N'-(4-fluorophenyl)malonamide 
• 864241-92-9 N-(4-Fluorophenyl)-N'-(4-{2-[(pyrrolidine-1-carbonyl)amino]pyridin-4-yloxy}phenyl)malonamide 
• 864245-62-5 Methyl 4-{3-fluoro-4-[2-(4-fluorophenylcarbamoyl)acetamino]phenoxy}pyridine-2-carboxylate 
• 864242-03-5 N-(2-fluoro-4-{2-[(morpholine-4-carbonyl)amino]pyridin-4-yloxy}phenyl)-N'-(4-fluorophenyl)malonamide 

Relevant academic research and scientific papers

Mild, efficient, and solvent-free synthesis of 4-hydroxy-2-quinolinones

Malonic acid monoanilides were obtained in excellent yield from the reaction of anilines with Meldrum's acid under solvent-free conditions. The malonic acid monoanilide intermediates were then treated with methanesulfonic acid anhydride (MSAA) to produce 4-hydroxy-2-quinolinones in excellent yield. It should be noted that both reactions had to be run under mild conditions to avoid the decarboxylation of the malonic acid monoanilide intermediate.

Cabozantinib preparation method

The invention discloses a cabozantinib preparation method. The target product cabozantinib is prepared by performing five-step reaction on diethyl malonate, 4-fluoroaniline, 4-chloro-6,7-dimethoxyquinoline, 4-aminophenol, 1,2-dibromoethane and the like us

Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7- oxo-7,8-dihydro-pyrido[2,3- d ]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5)

The success of imatinib, a BCR-ABL inhibitor for the treatment of chronic myelogenous leukemia, has created a great impetus for the development of additional kinase inhibitors as therapeutic agents. However, the complexity of cancer has led to recent interest in polypharmacological approaches for developing multikinase inhibitors with low toxicity profiles. With this goal in mind, we analyzed more than 150 novel cyano pyridopyrimidine compounds and identified structure-activity relationship trends that can be exploited in the design of potent kinase inhibitors. One compound, 8-cyclopentyl-2-[4-(4-methyl- piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6- carbonitrile (7x), was found to be the most active, inducing apoptosis of tumor cells at a concentration of approximately 30-100 nM. In vitro kinase profiling revealed that 7x is a multikinase inhibitor with potent inhibitory activity against the CDK4/CYCLIN D1 and ARK5 kinases. Here, we report the synthesis, structure-activity relationship, kinase inhibitory profile, in vitro cytotoxicity, and in vivo tumor regression studies by this lead compound.

Bioisosteric replacement of an acylureido moiety attached to an indolin-2-one scaffold with a malonamido or a 2/4-pyridinoylamido moiety produces a selectively potent Aurora-B inhibitor

Bioisosteric replacement of acylureido moiety in 6-acylureido-3- pyrrolylmethylidene-2-oxoindoline derivatives resulted in a series of malonamido derivatives with indolin-2-one scaffold (11-14). Further conformational restrictions of the malonamido moiety led to 2-oxo-1,2-dihydropyridine (21-25) or a 4-oxo-1,4-dihydropyridine derivatives (31-36). 4-Oxo-1,4-dihydropyridine derivatives were more potent Aurora B inhibitors than their 2-oxo-1,2- dihydropyridine counterparts and demonstrated cytotoxicities against A549 and HepG2 cells in the submicromolar range. In A549 cells, 31h decreased phosphorylation of histone H3, triggered polyploidy, induced expression of pro-apoptotic Fas and FasL with subsequent activation of caspase 8, resulting into apoptosis. In a Huh7-xenograft mouse model, 31h demonstrated potent in vivo efficacy with a daily dose of 5 mg/kg.

INDOLIN-2-ONE DERIVATIVES AS PROTEIN KINASE INHIBITORS

A novel class of indoline-2-one derivatives are disclosed. These compounds are protein kinase inhibitors which are useful for treating hyperproliferative diseases such as cancer.

N3-Arylmalonamides: A new series of thieno[3,2-b]pyridine based inhibitors of c-Met and VEGFR2 tyrosine kinases

A family of thieno[3,2-b]pyridine based small molecule inhibitors of c-Met and VEGFR2 were designed based on lead structure 2. These compounds were shown to have IC50 values in the low nanomolar range in vitro and were efficacious in human tumo

Heterobicyclic thiophene compounds and methods of use

Compounds of Formula I and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula I and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

BENZENESULFONAMIDE COMPOUNDS AND THEIR USE AS BLOCKERS OF CALCIUM CHANNELS

The invention relates to piperidinyl and hexahydroazepinyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1-R3, Z and q are defined as set forth in the specification. The inve

Bicyclic heterocycles as kinase inhibitors

The compounds of the instant invention can be used as anticancer agents. More specifically, the invention comprises a compound having Formula I or II,