285984-22-7

Usage

Uses

Used in Pharmaceutical Industry:
(4-HYDROXY-NAPHTHALEN-1-YL)-CARBAMIC ACID TERT-BUTYL ESTER is used as a chemical intermediate for the synthesis of certain pharmaceuticals, leveraging its carbamate and naphthalene structures to contribute to the development of new drugs.
Used in Agrochemical Industry:
In the agrochemical sector, (4-HYDROXY-NAPHTHALEN-1-YL)-CARBAMIC ACID TERT-BUTYL ESTER is utilized as a precursor in the production of agrochemicals, potentially enhancing crop protection and management through its chemical properties.
Used in Research Applications:
(4-HYDROXY-NAPHTHALEN-1-YL)-CARBAMIC ACID TERT-BUTYL ESTER serves as a valuable research tool in chemical and material science, where its unique structure and reactivity can be explored for new discoveries and innovations in various fields.

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 5959-56-8 4-amino-1-naphthol hydrochloride 
• 86-57-7 1-Nitronaphthalene 
• 605-62-9 4-nitro-1-naphthol 
• 2834-90-4 4-amino-1-naphthol 

Relevant academic research and scientific papers

POLYAROMATIC UREA DERIVATIVES AND THEIR USE IN THE TREATMENT OF MUSCLE DISEASES

The current invention provides urea derivatives, in particular compounds having the core structure heteroaryl-NH-CO-NH-aryl-O- heteroaryl, for use in treating, ameliorating, delaying, curing and/ or preventing a disease or condition associated with muscle cells and/or satellite cells, such as Duchenne muscular dystrophy, Becker muscular dystrophy, cachexia or sarcopenia.

Tuning Tetrazole Photochemistry for Protein Ligation and Molecular Imaging

Photochemistry provides a wide range of alternative reagents that hold potential for use in bimolecular functionalisation of proteins. Here, we report the synthesis and characterisation of metal ion binding chelates derivatised with disubstituted tetrazoles for the photoradiochemical labelling of monoclonal antibodies (mAbs). The photophysical properties of tetrazoles featuring extended aromatic systems and auxochromic substituents to tune excitation toward longer wavelengths (365 and 395 nm) were studied. Two photoactivatable chelates based on desferrioxamine B (DFO) and the aza-macrocycle NODAGA were functionalised with a tetrazole and developed for protein labelling with 89Zr, 64Cu and 68Ga radionuclides. DFO-tetrazole (1) was assessed by direct conjugation to formulated trastuzumab and subsequent radiolabelling with 89Zr. Radiochemical studies and cellular-based binding assays demonstrated that the radiotracer remained stable in vitro retained high immunoreactivity. Positron emission tomography (PET) imaging and biodistribution studies were used to measure the tumour specific uptake and pharmacokinetic profile in mice bearing SK-OV-3 xenografts. Experiments demonstrate that tetrazole-based photochemistry is a viable approach for the light-induced synthesis of PET radiotracers.

Discovery of 2-oxy-2-phenylacetic acid substituted naphthalene sulfonamide derivatives as potent KEAP1-NRF2 protein-protein interaction inhibitors for inflammatory conditions

Nuclear factor erythroid 2-related factor 2 (NRF2) is a pleiotropic transcription factor which regulates the constitutive and inducible transcription of a wide array of genes and confers protection against a variety of pathologies. Directly disrupting Kelch-like ECH-associated protein 1 (KEAP1)-NRF2 protein-protein interaction (PPI) has been explored as a promising strategy to activate NRF2. We reported here the first identification of a series of 2-oxy-2-phenylacetic acid substituted naphthalene sulfonamide derivatives as potent KEAP1-NRF2 inhibitors. Our efforts led to the potent small molecule KEAP1-NRF2 inhibitor, 20c, which exhibited a Kd of 24 nM to KEAP1 and an IC50 of 75 nM in disrupting KEAP1-NRF2 interaction. Subsequent biological studies provided consistent evidence across mouse macrophage cell-based and in vivo models that 20c induced NRF2 target gene expression and enhanced downstream antioxidant and anti-inflammatory activities. Our study not only demonstrated that small molecule KEAP1-NRF2 PPI inhibitors can be potential preventive and therapeutic agents for diseases and conditions involving oxidative stress and inflammation but also enriched the chemical diversity of the KEAP1-NRF2 inhibitors.

Naphthylamine compound and biologically acceptable salt thereof as well as preparation method and application thereof

Aiming at shortage of anti-cancer targeting medicines in the prior art, the invention provides a naphthylamine compound and a biologically acceptable salt thereof as well as a preparation method and application thereof. By adopting the naphthylamine compo

1-sulfonamide-4-aryloxy compound, preparation method and medical application of 1-sulfonamide-4-aryloxy compound

The invention relates to the field of medicinal chemistry, in particular to a compound (I) with 1-sulfonamide-4-aryloxy being a basis framework. The compound has anti-inflammatory activity. A primary activity test proves that the compound has good interference Keap1-Nrf2 combination, so that Nrf2 is activated, and the compound has potential anti-inflammatory activity and can be used for treating numerous inflammation-related diseases including the chronic obstructive pulmonary disease (COPD), the Alzheimer's disease, Parkinson, atherosclerosis, the chronic renal disease (CKD), diabetes, intestine inflammations, rheumatoid arthritis and the like. (Please see the description for the formula I.).

Iminium ion catalysis: The enantioselective Friedel-Crafts alkylation-acetalization cascade of naphthols with α,β-unsaturated cyclic ketones

The first enantioselective Friedel-Crafts alkylation-acetalization-cascade of naphthols with α,β-unsaturated cyclic ketones and 1H-inden-1-ones was realized. 9-Amino(9-deoxy)epi-quinine A was the catalyst of choice for the realization of polycyclic structures with high enantiocontrol.

Development of a fluorescent-tagged kinase assay system for the detection and characterization of allosteric kinase inhibitors

Kinase disregulation disrupts the intricate network of intracellular signaling pathways and contributes to the onset of diseases such as cancer. Although several kinase inhibitors are on the market, inhibitor selectivity and drug resistance mutations persist as fundamental challenges in the development of effective long-term treatments. Chemical entities binding to less conserved allosteric sites would be expected to offer new opportunities for scaffold development. Because no high-throughput method was previously available, we developed a fluorescence-based kinase binding assay for identifying and characterizing ligands which stabilize the inactive kinase conformation. Here, we present a description of the development and validation of this assay using the serine/threonine kinase p38R. By covalently attaching fluorophores to the activation loop of the kinase, we were able to detect conformational changes and measure the Kd, kon, and koff associated with the binding and dissociation of ligands to the allosteric pocket. We report the SAR of a synthesized focused library of pyrazolourea derivatives, a scaffold known to bind with high affinity to the allosteric pocket of p38R. Additionally, we used protein X-ray crystallography together with our assay to examine the binding and dissociation kinetics to characterize potent quinazoline- and quinoline-based type II inhibitors, which also utilize this binding pocket in p38α. Last, we identified the b-Raf inhibitor sorafenib as a potent low nanomolar inhibitor of p38α and used protein X-ray crystallography to confirm a unique binding mode to the inactive kinase conformation.

SUBSTITUTED PYRAZOLE COMPOUNDS USEFUL AS SOLUBLE EPOXIDE HYDROLASE INHIBITORS

Disclosed are compounds active against soluble epoxide hydrolase (sEH), compositions thereof and methods of using and making same.

1,4-DISUBSTITUTED NAPHTALENES AS INHIBITORS OF P38 MAP KINASE

In general, the present invention relates to compounds capable of inhibiting P38, methods for inhibiting P38 in vivo or in vitro, diagnostics for determining activity in the treatment of P38 and/or cytokine-associated conditions and methods for treating c

SILICON COMPOUNDS AND THEIR USE

A compound of formula (1) wherein R1, R2 and R3 are the same or different and are each alkyl, -alkyl-aryl or -alkyl-cycloalkyl; or R1-Si-R 2 taken together form heterocycloalkyl; R4 is aryl