175968-61-3

Usage

Uses

Used in Pharmaceutical Industry:
4-(benzyloxy)-3-fluorobenzaldehyde serves as a key intermediate in the synthesis of pharmaceuticals, leveraging its reactivity to form complex molecular structures that can exhibit therapeutic properties. Its contribution to the development of new drugs is significant, particularly in the creation of molecules with specific binding affinities and pharmacological activities.
Used in Agrochemical Industry:
In the agrochemical sector, 4-(benzyloxy)-3-fluorobenzaldehyde is utilized as a precursor in the production of various agrochemicals. Its role in this industry is crucial for the synthesis of compounds that can be used in pest control, crop protection, and other agricultural applications, thereby enhancing crop yields and quality.
Used in Fine Chemicals Industry:
4-(benzyloxy)-3-fluorobenzaldehyde is also employed in the synthesis of fine chemicals, which are high-purity chemicals used in various applications such as fragrances, dyes, and other specialty chemicals. Its versatility allows for the production of a wide array of compounds with specific properties tailored to meet the demands of different industries.
Used as a Building Block in Organic Synthesis:
Beyond specific industries, 4-(benzyloxy)-3-fluorobenzaldehyde is recognized as a building block in organic synthesis. Its aromatic structure and functional groups make it an ideal starting material for the construction of more complex organic molecules, which can be further utilized in research and development for new materials and compounds with unique properties.

Upstream product

• 405-05-0 3-fluoro-4-hydroxybenzaldehyde 
• 100-39-0 benzyl bromide 
• 100-44-7 benzyl chloride 
• 1044067-62-0 4-(benzyloxy)-3-fluorobenzonitrile 
• 351-54-2 3-fluoro-p-anisaldehyde 
• 100-51-6 benzyl alcohol 
• 405-04-9 3-fluoro-4-hydroxybenzonitrile 
• 4394-85-8 4-morpholinecarboxaldehyde 
• 133057-82-6 1-benzyloxy-4-bromo-2-fluorobenzene 

Downstream Products

• 536974-94-4 [4-(benzyloxy)-3-fluorophenyl]methanol 
• 638214-82-1 ethyl (2E)-3-{3-fluoro-4-[(phenylmethyl)oxy]phenyl}-2-propenoate 
• 872030-46-1 6-benzyloxy-5-fluoro-1H-indole-2-carboxylic acid methyl ester 
• 1240308-56-8 1-(4-(benzyloxy)-3-fluorobenzyl)azetidine-3-carboxylic acid 
• 1337991-95-3 2-(4-benzyloxy-3-fluorophenyl)-4-bromo-5-propyltetrahydropyran 
• 839694-31-4 methyl 3-(4-(benzyloxy)-3-fluorophenyl)acrylate 
• 668478-41-9 [rac]-3-(4-benzyloxy-3-fluoro-phenyl)-2-isopropoxy-propionic acid ethyl ester 
• 94139-03-4 ethyl 3-(3-fluoro-4-hydroxyphenyl)-2-propanoate 

Relevant academic research and scientific papers

BIFUNCTION CHEMICAL EPIGENENTIC MODIFIERS AND METHODS OF USE

The present disclosure relates to bifunctional chemical epigenetic modifiers, and methods of making, kits and using the bifunctional chemical epigenetic modifiers. The bifunctional chemical epigenetic modifiers can include a FK506 molecule or derivative thereof, a linker and a bifunctional ligand. The bifunctional ligand can be a histone deacetylase inhibitor.

PIM KINASE INHIBITOR COMPOSITIONS AND USES THEREOF

This disclosure relates to compounds and compositions useful as inhibitors of PIM kinases. Also provided are methods of synthesis and methods of use of PIM inhibitors in treating individuals suffering from cancerous malignancies.

RNAI AGENTS FOR INHIBITING EXPRESSION OF HIF-2 ALPHA (EPAS1), COMPOSITIONS THEREOF, AND METHODS OF USE

The present disclosure relates to RNAi agents, for example, double stranded RNAi agents, able to inhibit HIF-2 alpha ( EPAS1 ) gene expression. Also disclosed are pharmaceutical compositions that include HIF-2 alpha RNAi agents and methods of use thereof. The HIF-2 alpha RNAi agents disclosed herein may be linked or conjugated to targeting ligands (such as compounds that have affinity for integrins, including alpha-v-beta-3 and alpha-v-beta-5 integrins) and pharmacokinetic (PK) enhancers, to facilitate the delivery to cells and tissues, including to clear cell renal cell carcinoma (ccRCC) cells and tumors. Delivery of compositions comprising the HIF-2 alpha RNAi agents in vivo provides for inhibition of HIF-2 alpha gene expression. The HIF-2 alpha RNAi agents can be used in methods of treatment of various diseases and disorders, including ccRCC.

EP300/CREBBP INHIBITOR

The present invention provides a compound having excellent histone acetyltransferase inhibitory activity against EP300 and/or CREBBP, or a pharmacologically acceptable salt thereof. The compound is represented by the following formula (1) or a pharmacologically acceptable salt thereof: wherein ring Q1, ring Q2, R1, R2, R3 and R4 respectively have the same meanings as defined in the specification.

LEUKOTRIENE SYNTHESIS INHIBITORS

Provided are specific leukotriene synthesis inhibitor compounds and pharmaceutical compositions comprising the compounds and methods of using the compounds and the pharmaceutical compositions in treating, for example, inflammatory diseases or conditions.

Structure-Activity Relationships of cyclo(l -Tyrosyl- l -tyrosine) Derivatives Binding to Mycobacterium tuberculosis CYP121: Iodinated Analogues Promote Shift to High-Spin Adduct

A series of analogues of cyclo(l-tyrosyl-l-tyrosine), the substrate of the Mycobacterium tuberculosis enzyme CYP121, have been synthesized and analyzed by UV-vis and electron paramagnetic resonance spectroscopy and by X-ray crystallography. The introduction of iodine substituents onto cyclo(l-tyrosyl-l-tyrosine) results in sub-μM binding affinity for the CYP121 enzyme and a complete shift to the high-spin state of the heme FeIII. The introduction of halogens that are able to interact with heme groups is thus a feasible approach to the development of next-generation, tight binding inhibitors of the CYP121 enzyme, in the search for novel antitubercular compounds.

Aromatic cyclopropyl amine compound, pharmaceutically acceptable salts thereof, and preparation method and application thereof

The invention relates to an aromatic cyclopropyl amine compound shown in a general formula (I) and pharmaceutically acceptable salts thereof, and preparation method of the compound and application thereof to the preparation of medicamentd for prevention o

Discovery of A-971432, an orally bioavailable selective sphingosine-1-phosphate receptor 5 (S1P5) agonist for the potential treatment of neurodegenerative disorders

S1P5 is one of 5 receptors for sphingosine-1-phosphate and is highly expressed on endothelial cells within the blood-brain barrier, where it maintains barrier integrity in in vitro models (J. Neuroinflamm. 2012, 9, 133). Little more is known about the effects of S1P5 modulation due to the absence of tool molecules with suitable selectivity and drug-like properties. We recently reported that molecule A-971432 (Harris et al., 2010) (29 in this paper) is highly efficacious in reversing lipid accumulation and age-related cognitive decline in rats (Van der Kam, et al., AAIC 2014). Herein we describe the development of a series of selective S1P5 agonists that led to the identification of compound 29, which is highly selective for S1P5 and has excellent plasma and CNS exposure after oral dosing in preclinical species. To further support its suitability for in vivo studies of S1P5 biology, we extensively characterized 29, including confirmation of its selectivity in pharmacodynamic assays of S1P1 and S1P3 function in rats. In addition, we found that 29 improves blood-brain barrier integrity in an in vitro model and reverses age-related cognitive decline in mice. These results suggest that S1P5 agonism is an innovative approach with potential benefit in neurodegenerative disorders involving lipid imbalance and/or compromised blood-brain barrier such as Alzheimer's disease or multiple sclerosis.

Synthesis, biological activity and structure-activity relationships of new benzoic acid-based protein tyrosine phosphatase inhibitors endowed with insulinomimetic effects in mouse C2C12 skeletal muscle cells

Insulin resistance is a complex altered metabolic condition characterized by impaired insulin signaling and implicated in the pathogenesis of serious human diseases, such as diabetes, obesity, neurodegenerative pathologies. In pursuing our aim to identify new agents able to improve cellular insulin sensitivity, we have synthesized new 4-[(5-arylidene-4-oxo-2-phenylimino/ oxothiazolidin-3-yl)methyl]benzoic acids (5, 8) and evaluated their inhibitory activity towards human protein tyrosine phosphatases PTP1B, LMW-PTP and TCPTP, enzymes which are involved in the development of insulin resistance. Compounds 5 and 8 showed from moderate to significant selectivity toward PTP1B over both the highly homologous TCPTP and the two isoforms of human LMW-PTP. In addition, most of the tested compounds selectively inhibited LMW-PTP IF1 over the isoform IF2. Docking studies into the active sites of PTP1B and LMW-PTP aided the rationalization of the observed PTP inhibitory profile. Moreover, most tested compounds were capable to induce the insulin metabolic pathway in mouse C2C12 skeletal muscle cells by remarkably stimulating both IRβ phosphorylation and 2-deoxyglucose cellular uptake.

2-(HETERO)ARYL-BENZIMIDAZOLE AND IMIDAZOPYRIDINE DERIVATIVES AS INHIBITORS OF ASPARAGIME EMETHYL TRANSFERASE

Substituted benzimidazole and 3H-imidazo[4,5-b]pyridines or formula I: where X and Y respectively are selected from: (i) N and N; and (ii) N and CR4; A2 is selected from:, a C5 heteroarylene group, containing 2 or 3 ring heteroatoms, where the bonds to L1 and the core are β to one another; L1 is selected from: (i)A1-O-CH2-A2; (ii)A1-CH2-O-A2; (iii)A1-C(=O)-NH-A2; (iv)A1-CH(OH)-A2; (v)A1-CH2-NH-C(=O)-A2; (vi) A1-S-CH2-A2; (vii)A1- CH2-S-A2; (viii)A1-CH2-A2; and (ix)A1-CH(CH3)-O-A2; A1 is phenyl, optionally substituted by F or CF3; their use as pharmaceuticals, and in particular, in treating cancer and hemoglobinopathies.