4983-28-2

Usage

Uses

Used in Pharmaceutical Industry:
2-Chloro-5-hydroxypyrimidine is used as a chemical intermediate for the synthesis of tandospirone derivatives, which possess anxiolytic (anxiety-reducing) activities. These derivatives are beneficial in the treatment of anxiety disorders and related conditions, providing relief and improving the quality of life for patients.
The anxiolytic properties of tandospirone derivatives are attributed to their ability to modulate the serotonin system in the brain, which is closely associated with mood regulation and anxiety. By acting on specific serotonin receptors, these compounds can help alleviate anxiety symptoms and provide a calming effect.

Upstream product

• 56622-03-8 2-Chloro-5-(dimethylaminomethyleneamino)pyrimidine 
• 22536-65-8 2-chloro-5-methoxy-pyrimidine 
• 56621-90-0 2-chloro-5-aminopyrimidine 
• 1003845-06-4 (2-chloropyrimidin-5-yl)boronic acid 

Downstream Products

• 138274-14-3 5-(benzyloxy)-2-chloropyrimidine 
• 1192813-64-1 2-chloro-5-(difluoromethoxy)pyrimidine 
• 82153-68-2 2-chloro-5-ethoxypyrimidine 
• 1350730-12-9 2-chloro-5-(3-(pyrrolidin-1-yl)phenoxy)pyrimidine 
• 1580440-61-4 2-chloro-5-(4-fluorophenoxy)pyrimidine 
• 1453211-57-8 2-chloro-5-[(3,5-dimethoxyphenyl)methoxy]pyrimidine 
• 1453211-61-4 2-chloro-5-[(2,6-difluoro-3,5-dimethoxyphenyl)methoxy]pyrimidine 
• 1453211-59-0 2-chloro-5-[1-(3,5-dimethoxyphenyl)ethoxy]pyrimidine 
• 1453207-63-0 5-[(2,6-difluorobenzyl)oxy]-N-{3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}pyrimidin-2-amine 
• 1453211-58-9 2-chloro-5-[(2,6-dichloro-3,5-dimethoxybenzyl)oxy]pyrimidine 
• 1453211-80-7 2-chloro-5-(1-(2,6-dichloro-3,5-dimethoxyphenyl)ethoxy)pyrimidine 

Relevant academic research and scientific papers

Preparation method of 2-chloro-5-hydroxypyrimidine

The invention relates to a preparation method of 2-chloro-5-hydroxypyrimidine. The preparation method is characterized by comprising the following steps: step a, adding 2-chloro-5-methoxypyrimidine and an organic acid solvent in a reaction vessel, stirring uniformly, adding hydrobromic acid and methionine, and stirring and heating for carrying out reflux reaction for 3-8 hours; step b, cooling toroom temperature after the reaction, adding water, carrying out solvent extraction several times, and merging organic phases; step c, washing and drying the organic phases, and then concentrating andpurifying to obtain a pale yellow solid target product. The preparation method has the beneficial effects that the ratio of raw materials is optimized, so that the impurity content of the product is significantly reduced; a hydrobromic acid-methionine system replaces boron tribromide for performing demethylation reaction, so that the cost of the raw materials is effectively reduced, and the product purity and the reaction yield are greatly improved.

FGFR4 INHIBITORS

Methods, compounds, pharmaceutical compositions, and methods of preparing medicaments for treating hepatocellular carcinoma having an altered FGFR4 and/or FGF19 status.

Orally Bioavailable Metal Chelators and Radical Scavengers: Multifunctional Antioxidants for the Coadjutant Treatment of Neurodegenerative Diseases

Neurodegenerative diseases are associated with oxidative stress that is induced by the presence of reactive oxygen species and the abnormal cellular accumulation of transition metals. Here, a new series of orally bioavailable multifunctional antioxidants (MFAO-2s) possessing a 2-diacetylamino-5-hydroxypyrimidine moiety is described. These MFAO-2s demonstrate both free radical and metal attenuating properties that are similar to the original published MFAO-1s that are based on 1-N,N′-dimethylsulfamoyl-1-4-(2-pyrimidyl)piperazine. Oral bioavailability studies in C57BL/6 mice demonstrate that the MFAO-2s accumulate in the brain at significantly higher levels than the MFAO-1s while achieving similar neural retina levels. The MFAO-2s protect human neuroblastoma and retinal pigmented epithelial cells against hydroxyl radicals in a dose-dependent manner by maintaining cell viability and intracellular glutathione levels. The MFAO-2s outperform clioquinol, a metal attenuator that has been investigated for the treatment of Alzheimer's disease.

NEUROPROTECTIVE MULTIFUNCTIONAL ANTIOXIDANTS AND THEIR MONOFUNCTIONAL ANALOGS

The neuroprotective multifunctional antioxidants are compounds that contain a 2-diacetylamino-5-hydroxypyrimidine moiety, having the structural formula: wherein R1 is CH2 or C2H4; R2 is H or —OR4 where R4 is H or aryl; and R3a and R3b are independently selected from the group consisting of H and —O-alkyl. The antioxidants are orally bioavailable metal-attenuating multifunctional antioxidants that can independently attenuate transition metals, as well as scavenger free radicals. The multifunctional antioxidant compounds, by their ability to independently chelate metals, such as Fe, Cu or Zn, and scavenge free radicals generated from different sources, are neuroprotective and are beneficial for the treatment of various neurological disorders, such as Alzheimer's disease, Parkinson's disease, ALS, traumatic brain injury, ocular disorders, such as cataract, glaucoma, age-related macular degeneration and other retinal degeneration, as well as for reducing the progression of diabetic complications.

TYROSINE KINASE INHIBITORS

The present invention relates to pyridazin-4(1H)-one derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

PYRROLIDINE GPR40 MODULATORS

The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR40 G protein-coupled receptor modulators which may be used as medicaments.

Multifunctional antioxidants for the treatment of age-related diseases

Analogues of N,N-dimethyl-4-(pyrimidin-2-yl)piperazine-1-sulfonamide possessing a free radical scavenger group (FRS), chelating groups (CHL), or both (FRS + CHL) have been synthesized. Electrospray ionization mass spectrometry studies indicate that select

HETEROCYCLIC COMPOUNDS AND METHODS OF USE

In one aspect, the present invention provides for a compound of Formula I; in which the variable X1a, X1b, X1c, X1d, Q, A, R1, B, L, E, and the subscripts m and n have the meanings as described herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.