82625-25-0

Upstream product

• 632-02-0 3-chloropropyl p-toluenesulfonate 
• 123-08-0 4-hydroxy-benzaldehyde 
• 142-28-9 1,3-Dichloropropane 
• 109-70-6 1.3-chlorobromopropane 
• 111627-46-4 4-(3-chloropropoxy)benzonitrile 
• 121-33-5 vanillin 

Downstream Products

• 114980-24-4 (E)-2-<2-<4-(3-chloropropoxy)phenyl>ethenyl>benzoxazole 
• 114980-25-5 (E)-2-<2-<4-(3-chloropropoxy)phenyl>ethenyl>benzothiazole 
• 124941-94-2 5-Chloro-2-{(E)-2-[4-(3-chloro-propoxy)-phenyl]-vinyl}-benzothiazole 
• 124941-85-1 2-{(E)-2-[4-(3-Chloro-propoxy)-phenyl]-vinyl}-6-methoxy-benzooxazole 
• 103108-01-6 4-(3-chloropropoxy)benzaldehyde ethylene acetal 
• 82625-46-5 4-(3-(piperidin-1-yl)propoxy)benzaldehyde 
• 398474-02-7 1-[4-(3-chloropropoxy)benzyl]piperidine 
• 915920-46-6 4-[3-(4-methyl-piperazin-1-yl)-propoxy]-benzaldehyde 
• 929532-57-0 (4R,5R)-2-[4-(3-chloropropoxy)phenyl]-4,5-diphenyl-1,3-dioxolane 
• 929532-56-9 (4S,5S)-2-[4-(3-chloropropoxy)phenyl]-4,5-diphenyl-1,3-dioxolane 
• 929219-25-0 4,5-bis(4-fluorophenyl)-2-[4-(3-chloropropoxy)phenyl]-1,3-dioxolane 
• 929219-24-9 4,5-bis(2-chlorophenyl)-2-[4-(3-chloropropoxy)phenyl]-1,3-dioxolane 
• 1012306-96-5 [3-(4-formylphenoxy)propyl]trimethylammonium chloride 
• 1202245-45-1 C₃₀H₂₃ClO₂ 

Relevant academic research and scientific papers

A Versatile Sub-Nanomolar Fluorescent Ligand Enables NanoBRET Binding Studies and Single-Molecule Microscopy at the Histamine H3Receptor

The histamine H3 receptor (H3R) is considered an attractive drug target for various neurological diseases. We here report the synthesis of UR-NR266, a novel fluorescent H3R ligand. Broad pharmacological characterization revealed UR-NR266 as a sub-nanomolar compound at the H3R with an exceptional selectivity profile within the histamine receptor family. The presented neutral antagonist showed fast association to its target and complete dissociation in kinetic binding studies. Detailed characterization of standard H3R ligands in NanoBRET competition binding using UR-NR266 highlights its value as a versatile pharmacological tool to analyze future H3R ligands. The low nonspecific binding observed in all experiments could also be verified in TIRF and confocal microscopy. This fluorescent probe allows the highly specific analysis of native H3R in various assays ranging from optical high throughput technologies to biophysical analyses and single-molecule studies in its natural environment. An off-target screening at 14 receptors revealed UR-NR266 as a selective compound.

Design, synthesis and biological evaluation of 2-styryl-5-hydroxy-4-pyrone derivatives and analogues as multiple functional agents with the potential for the treatment of Alzheimer's disease

A novel series of 2-styryl-5-hydroxy-4-pyrone derivatives and analogues were designed and synthesized as H3 receptor antagonism based multitarget-directed ligands (MTDLs) for AD therapy using pharmacophore-combine strategy. The 2-styryl-5-hydro

Design, synthesis, and evaluation of some novel biphenyl imidazole derivatives for the treatment of Alzheimer's disease

The multi-targeted organized strategy provides effectual and significant results to cure progressive neurodegenerative diseases like AD. Treatment for this awful disease is in infancy till now. A series of novel 4, 5-diphenyl-1H-imidazole linked piperazin

HYPOXANTHINE COMPOUND

PROBLEM TO BE SOLVED: To provide a novel compound having an inhibitory action of prolyl hydroxylase (PHDs) and useful as a therapeutic agent of an inflammatory bowel disease such as ulcerative colitis. SOLUTION: The present invention relates to a hypoxanthine compound represented by the following formula (I) or a pharmacologically acceptable salt thereof. The compound of the present invention or its pharmaceutically acceptable salt has an inhibitory effect of prolyl hydroxylase and is useful as a therapeutic agent for inflammatory bowel disease such as ulcerative colitis. SELECTED DRAWING: None COPYRIGHT: (C)2021,JPOandINPIT

Controlled Reduction of Nitriles by Sodium Hydride and Zinc Chloride

A new protocol for the controlled reduction of nitriles to aldehydes was developed using a combination of sodium hydride and zinc chloride. The iminyl zinc intermediates derived from aromatic nitriles could be further functionalized with allylmetal nucleophiles to afford homoallylamines. As the method allows the reduction of various aliphatic and aromatic nitriles with a concise procedure under milder reaction conditions and exhibits wide functional group compatibility, it is well suited for use in various opportunities in chemical synthesis.

Design, synthesis and biological evaluation of novel 4-anlinoquinazoline derivatives as EGFR inhibitors with the potential to inhibit the gefitinib-resistant nonsmall cell lung cancers

A series of quinazoline derivatives with benzylidene hydrazine carboxamide were designed and synthesised as EGFR inhibitors. Most compounds exhibited exceptional anti-proliferative activity against A549, HepG2, MCF-7 and H1975 cells. Furthermore, six compounds demonstrated excellent inhibition activity against EGFRWT with the IC50 value both less than 2 nM. Among the six compounds, 44 exhibited the strongest activity (0.4 nM) and potently inhibited EGFRL858R/T790M (0.1 μM). Excitingly, the most potent compound 14 showed excellent enzyme inhibitory activity with 6.3 nM and 8.4 nM for both EGFRWT and EGFRT790M/L858R. The result of AO single staining and Annexin V/PI staining showed that the compound 14 and 44 could induce remarkable apoptosis of A549 cells. The compound 14 arrested the cell cycle at the S phase and compound 44 arrested the cell cycle at the G0 phase in A549 cells. These preliminary results demonstrate that compound 14 and 44 may be promising lead compound-targeting EGFR.

Preparation and applications of phenylquinolinone-based and flavone-based derivative

The present invention relates to a phenylquinolinone-based and flavone-based derivative and a preparation method thereof, wherein the derivative is a histamine H3 receptor antagonist, can protect andrestore the normal function of central nervous system, e

An efficient multigram-scale synthesis of 4-(ω-chloroalkoxy)phenols

Efficient multigram two-step syntheses of 4-(2-chloroethoxy)phenol and 4-(3-chloropropoxy)phenol in >70% yields starting from 4-hydroxybenzaldehyde and reagents with general formula Cl(CH2)nX (X = Cl, n = 2; X = OTs, n = 3) are proposed. 4-(2-Chloroethoxy)phenol can also be conveniently prepared from 4-methoxyphenol and 1,2-dichloroethane. The compounds thus obtained can be used in carbohydrate chemistry to synthesize glycosides bearing "universal" 4-(ω-chloroalkoxy)phenyl aglycons.

Imidazolium salt-supported Mukaiyama reagent: An efficient condensation reagent for amide bond formation

A novel imidazolium salt-supported Mukaiyama reagent (2-chloropyridinium salt) has been developed and explored as an efficient coupling agent for amide bond formation. The use of an ionic liquid-supported reagent enabled isolation of the amide products by simple extraction with organic solvents in high purity and avoiding column chromatography purification. This journal is

Design, synthesis and anticholinesterase activity of novel benzylidenechroman-4-ones bearing cyclic amine side chain

A series of 3-(4-(aminoalkoxy)benzylidene)-chroman-4-ones 7a-r were designed and synthesized as analogs of homoisoflavonoids which are well known natural products with diverse pharmacological properties related to Alzheimer's disease. The in vitro anti-cholinesterase activity of designed compounds 7a-r against AChE and BuChE, revealed that compounds bearing piperidinylethoxy residue showed potent activity against AChE at sub-micromolar level (IC50 values = 0.122-0.207 μM), more potent than reference drug tacrine. The structure-activity relationships study of piperidinylethoxy series demonstrated that the selectivity and physicochemical properties of compounds could be optimized by selection of a proper substituent on the C-7 position of chroman ring, while the high potency of the molecule against AChE was reserved.