79996-99-9

Usage

Uses

Used in Organic Synthesis:
1-BROMO-4-(BROMOMETHYL)NAPHTHALENE is used as a brominating agent for various organic synthesis processes, facilitating the introduction of bromine atoms into organic molecules, which can enhance their reactivity and properties.
Used in Pharmaceutical Synthesis:
In the pharmaceutical industry, 1-BROMO-4-(BROMOMETHYL)NAPHTHALENE is used as a key intermediate in the synthesis of various drugs, contributing to the development of new medications with improved therapeutic effects.
Used in Agrochemical Production:
1-BROMO-4-(BROMOMETHYL)NAPHTHALENE is employed in the production of agrochemicals, such as pesticides and herbicides, to enhance their effectiveness in controlling pests and weeds in agricultural settings.
Used in Fluorescent Dye Manufacturing:
1-BROMO-4-(BROMOMETHYL)NAPHTHALENE is utilized in the manufacturing of fluorescent dyes, which are essential in various applications, including bioimaging, diagnostics, and as markers in research and development.
Used in Specialty Chemicals Production:
1-BROMO-4-(BROMOMETHYL)NAPHTHALENE is also used in the production of specialty chemicals, which have unique properties and applications in industries such as plastics, coatings, and textiles.

Upstream product

• 50-00-0 formaldehyd 
• 90-11-9 1-Bromonaphthalene 
• 6627-78-7 1-bromo-4-methylnaphthalene 
• 7726-95-6 bromine 
• 16650-55-8 4-bromonaphthalene-1-carboxylic acid 
• 90-12-0 1-Methylnaphthalene 
• 46258-62-2 1-(4-bromonaphthalen-1-yl)ethanone 
• 288372-59-8 1-allyldimethylsilyl-4-bromonaphthalene 
• 83-53-4 1,4-dibromonaphthalene 
• 288372-60-1 1-allyldimethylsilyl-4-naphthalenemethanol 
• 75-15-0 carbon disulfide 
• 56052-26-7 (4-bromonaphthalen-1-yl)methanol 
• 3163-27-7 2-(bromomethyl)naphthalene 

Downstream Products

• 50672-84-9 4-bromo-1-naphthaldehyde 
• 35615-97-5 4-bromo-naphthalene-1-carboxylic acid methyl ester 
• 1234382-25-2 5-(3,5-dichloro-phenyl)-5-trifluoromethyl-3-(4-trimethylsilanylethynyl-naphthalen-1-yl)-4,5-dihydro-isoxazole 
• 1234381-54-4 5-(3,5-dichloro-phenyl)-3-{4-[1-(2,2,2-trifluoro-ethyl)-1H-pyrazol-4-yl]-naphthalen-1-yl}-5-trifluoromethyl-4,5-dihydro-isoxazole 
• 1234381-72-6 2-(4-{4-[5-(3,5-dichloro-phenyl)-5-trifluoromethyl-4,5-dihydro-isoxazol-3-yl]-naphthalen-1-yl}-[1,2,3]triazol-1-ylmethyl)-pyridine 
• 1234381-46-4 4-{4-[5-(3,5-dichloro-phenyl)-5-trifluoromethyl-4,5-dihydro-isoxazol-3-yl]-naphthalen-1-yl}-pyrazole-1-carboxylic acid tert-butyl ester 
• 1234381-53-3 5-(3,5-dichloro-phenyl)-3-[4-(1H-pyrazol-4-yl)-naphthalen-1-yl]-5-trifluoromethyl-4,5-dihydro-isoxazole 
• 1234382-26-3 5-(3,5-dichloro-phenyl)-3-(4-ethynyl-naphthalen-1-yl)-5-trifluoromethyl-4,5-dihydro-isoxazole 
• 943847-23-2 3-(4-bromo-1-naphthalenyl)-5-(3,5-dichlorophenyl)-4,5-dihydro-5-(trifluoromethyl)isoxazole 
• 92616-49-4 4-bromonaphthalene-1-carbonitrile 

Relevant academic research and scientific papers

Discovery of Novel Bicyclic Imidazolopyridine-Containing Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Improved Efficacy and Favorable Druggability

Lesinurad is a uricosuric agent for the treatment of hyperuricemia associated with gout, which was found lacking in efficacy and safety. Here, scaffold hopping and molecular hybridization were exploited to modify all the structural components of lesinurad, and 36 novel compounds bearing bicyclic imidazolopyridine core were obtained. In a mouse model of acute hyperuricemia, 29 compounds demonstrated increased serum uric acid (SUA)-reducing activity; SUA was treated with 12, 23, and 29 about fourfold lower compared with that of lesinurad. Moreover, 23 exhibited stronger URAT1 inhibition activity (IC50 = 1.36 μM) than lesinurad (IC50 = 5.54 μM). Additionally, 23 showed favorable safety profiles, and no obvious acute toxicity was observed in Kunming mice under a single dose of 1000 mg·kg-1. 23 also achieved excellent pharmacokinetic properties with the oral bioavailability of 59.3%. Overall, all the results indicated that 23 is a promising drug candidate in the treatment of hyperuricemia and gout.

A new 2D Cu-MOF constructed from carboxylate ligands containing C-H?π interactions as a recyclable responsive luminescent sensor for VOCs

A new type of 2D metal-organic framework (MOF), namely Cu-MOF, was constructed from Cu(NO3)2·3H2O and the novel ligand 1,4-bis(4-naphthoic acid)benzene. The C-H?π interactions in the Cu-MOF effectively reduced aggregation-caused quenching (ACQ) due to restrictions in intramolecular motion (RIM), increased fluorescence, and controlled crystal packing properties, resulting in low dimensional parallelogram channels and a responsive “turn-on” fluorescence. The activated Cu-MOF exhibited excellent chemical sensing properties to various volatile organic compounds (VOCs) and showed excellent recyclability.

CRYSTAL FORM OF URATE TRANSPORTER 1 INHIBITOR AND PREPARATION METHOD AND USE THEREOF

The present invention provides a crystal form of urate transporter 1 inhibitor and a preparation method and use thereof. The crystal form is characterized by a stable state of appearance and a capability of further improving the purity and storage stability of the compound, etc., and suitable as a pharmaceutical raw material.

COMPOUNDS FOR INHIBITION OF ALPHA 4β7 INTEGRIN

The present disclosure provides a compound of Formula (I); or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula (I), processes for preparing compounds of Formula (I), and therapeutic methods for treating inflammatory disease.

METHOD FOR PREPARING URATE TRANSPORTER 1 INHIBITOR

Provided is a method for preparing a URAT1 inhibitor, 2-((5-bromo-4-((4-bromonaphthalen-1-yl)methyl)-4H-1,2,4-triazol-3-yl)thio) acetic acid represented by the following formula ZXS-BR, the reaction equation of which being shown as follows. Compared with the prior art, the preparation method provided by the present application is of low cost, ease of handling, ease of quality control, and applicable to industrialization.

Carbocation Catalyzed Bromination of Alkyl Arenes, a Chemoselective sp3 vs. sp2 C?H functionalization.

The versatility of the trityl cation (TrBF4) as a highly efficient Lewis acid organocatalyst is demonstrated in a light induced benzylic brominaion of alkyl-arenes under mild conditions. The reaction was conducted at ambient temperature under common hood light (55 W fluorescent light) with catalyst loadings down to 2.0 mol% using N-bromosuccinimide (NBS) as the brominating agent. The protocol is applicable to an extensive number of substrates to give benzyl bromides in good to excellent yields. In contrast to most previously reported strategies, this protocol does not require any radical initiator or extensive heating. For electron-rich alkyl-arenes, the trityl ion catalyzed bromination could be easily switched between benzylic sp3 C?H functionalization and arene sp2 C?H functionalization by simply alternating the solvent. This chemoselective switch allows for high substrate control and easy preparation of benzyl bromides and bromoarenes, respectively. The chemoselective switch was also applied in a one-pot reaction of 1-methylnaphthalene for direct introduction of both sp3 C?Br and sp2 C?Br functionality. (Figure presented.).

Synthesis method of 4-bromonaphthalene-1-carbonitrile

The invention discloses a synthesis method of 4-bromonaphthalene-1-carbonitrile. The method comprises the following steps: 1, replacing hydrogen on 1-methyl naphthalene benzene ring with bromine by taking 1-methyl naphthalene as a raw material, so as to obtain 4-bromine-1-methyl naphthalene (I); 2, replacing hydrogen on the methyl of the 4-bromine-1-methyl naphthalene (I) with bromine to obtain 4-bromine-1-bromine methyl naphthalene (II); 3, carrying out a sommelet reaction on the 4-bromine-1-bromine methyl naphthalene (II) to obtain 4-bromine-1-naphthaldehyde (III); 4, oximating the 4-bromine-1-naphthaldehyde (III) to obtain 4-bromine-1-naphthaldehyde oxime (IV); 5, carrying out dehydration on the 4-bromine-1-naphthaldehyde oxime (IV) to obtain the 4-bromonaphthalene-1-carbonitrile (V). The synthesis method has the advantages of being reasonable in process route design, cheap and available in raw and auxiliary materials, high in yield, low in cost, suitable for industrial production, and the like.

COMPOUNDS FOR BINDING PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9 (PCSK9)

The present disclosure relates to novel compounds, methods, and compositions capable of binding to PCSK9, thereby modulating PCSK9 proprotein convertase enzyme activity. The compounds of the disclosure include compounds Formula (I).

A process for the preparation of halogenated aryl armor cyanogen (by machine translation)

The present invention provides a method for the preparation of halogenated aryl armor cyanogen, comprising the following steps, the structure of the compound of the formula IV, iodine in water after the reaction the solvent, the structure of formula I is the halogenated aryl armor cyanogen. Green of the present invention the process for the preparation of halogenated aryl armor cyanogen, the compound of the formula IV, the ammonia in the iodine directly after the reaction in a solvent, to obtain halogenated aryl armor cyanogen (halogenated aryl a cyanogen derivatives). The invention provides a simple process reaction route, mild condition, does not use the hypertoxic cuprous cyanide, relatively high purity and yield, and does not need to, microwave and measures to improve the yield, in terms of industrial production more practical; in addition, the present invention provides method for the preparation of, its corresponding post-treatment step is simple, is more suitable for large scale industrial production. (by machine translation)

Discovery of a flexible triazolylbutanoic acid as a highly potent uric acid transporter 1 (URAT1) inhibitor

In order to systematically explore and understand the structure-activity relationship (SAR) of a lesinurad-based hit (1c) derived from the replacement of the S atom in lesinurad with CH2, 18 compounds (1a-1r) were designed, synthesized and subjected to in vitro URAT1 inhibitory assay. The SAR exploration led to the discovery of a highly potent flexible URAT1 inhibitor, 1q, which was 31-fold more potent than parent lesinurad (IC50 = 0.23 μM against human URAT1 for 1q vs. 7.18 μM for lesinurad). The present study discovered a flexible molecular scaffold, as represented by 1q, which might serve as a promising prototype scaffold for further development of potent URAT1 inhibitors, and also demonstrated that the S atom in lesinurad was not indispensable for its URAT1 inhibitory activity.