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Usage

Uses

Used in Pharmaceutical Industry:
1-Fluoro-2,3-dimethoxybenzene is used as an intermediate in the synthesis of pharmaceuticals for its ability to contribute to the development of new drugs with specific therapeutic properties. Its presence in the molecular structure can influence the pharmacokinetics and pharmacodynamics of the resulting compounds, enhancing their efficacy and safety.
Used in Agrochemical Industry:
In the agrochemical sector, 1-Fluoro-2,3-dimethoxybenzene is utilized as an intermediate in the production of agrochemicals, such as pesticides and herbicides. Its incorporation into these compounds can improve their effectiveness in controlling pests and weeds, thereby increasing crop yields and protecting agricultural investments.
Used in Organic Synthesis:
1-Fluoro-2,3-dimethoxybenzene is used as a versatile building block in organic synthesis for its capacity to react with other chemicals, leading to the formation of new compounds with a range of properties and applications. This makes it a valuable component in the creation of specialty chemicals, materials, and other organic products.
Used as a Solvent:
1-FLUORO-2,3-DIMETHOXYBENZENE also serves as a solvent in various chemical processes due to its ability to dissolve a wide range of substances. Its use in this capacity facilitates reactions and can improve the efficiency of chemical synthesis, making it an important component in the production of various commercial products.

InChI:InChI=1/C8H9FO2/c1-10-7-5-3-4-6(9)8(7)11-2/h3-5H,1-2H3

Upstream product

• 91-16-7 1,2-dimethoxybenzene 
• 73943-41-6 2-fluoro-6-methoxyphenol 
• 77-78-1 dimethyl sulfate 
• 96994-70-6 2-fluoro-6-hydroxyanisole 
• 456-49-5 1-fluoro-3-methoxybenzene 
• 74266-68-5 fluoro-3 methoxy-2 benzaldehhyde 
• 363-52-0 3-fluorocatechol 
• 74-88-4 methyl iodide 
• 103731-48-2 N-fluoro-N-(exo-2-norbornyl)-p-toluenesulfonamide 

Downstream Products

• 363-52-0 3-fluorocatechol 
• 1716-43-4 α-chloro-2-fluoro-3,4-dimethoxytoluene 
• 37686-68-3 2-fluoro-3,4-dimethoxybenzaldehyde 
• 71924-61-3 3-fluoro-4,5-dimethoxybenzaldehyde 
• 5150-42-5 2,3-dimethoxyphenol 
• 158641-45-3 1-(2-fluoro-3,4-dimethoxyphenyl)ethanone 
• 73943-41-6 2-fluoro-6-methoxyphenol 
• 96994-70-6 2-fluoro-6-hydroxyanisole 
• 2967-96-6 2-fluoro-3,4-dimethoxybenzoic acid 
• 158641-49-7 4-Ethyl-3-fluoro-benzene-1,2-diol 
• 158641-47-5 1-Ethyl-2-fluoro-3,4-dimethoxy-benzene 
• 158641-53-3 2-Bromo-1-(2-fluoro-3,4-dimethoxy-phenyl)-ethanone 
• 158641-61-3 2-[2-(2-Fluoro-3,4-dihydroxy-phenyl)-2-oxo-ethyl]-isoindole-1,3-dione 
• 158641-55-5 2-fluoro-3,4-dimethoxy-ω-phthalimidoacetophenone 

Relevant academic research and scientific papers

QUINAZOLINE DERIVATIVES AS ANTITUMOR AGENTS

The present application relates to novel quinazoline compounds as inhibitors of type I receptor tyrosine kinases, the pharmaceutical compositions comprising one or more of the compounds and salts thereof as an active ingredient, and the use of the compounds and salts thereof in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals and especially in humans.

Synthesis of stable isotope labeled anacetrapib, its major metabolites and [14C]anacetrapib

Cholesteryl ester transfer protein inhibitors are an important class of compounds designed to treat hypocholesterolemia and prevent cardiovascular disease. Anacetrapib (MK-0859) is currently in phase III trials for the treatment of elevated cholesterol levels and prevention of cardiovascular disease. In order to further support the development of anacetrapib, we prepared [M + 6]MK-0859, which was required in support of an absolute bioavailability study of the active pharmaceutical ingredient (API). Additional support included the synthesis of an internal standard [M + 13] and three stable isotope labeled metabolites, which were used to analyze clinical samples, and [ 14C]MK-0859 to support drug metabolism studies. A labeling strategy for the preparation of [M + 6], [M + 13], and [14C]anacetrapib is described. The preparation of stable isotope labelled metabolites of anacetrapib is also described.

ANTIBACTERIAL COMPOUNDS

The present Invention relates to cephalosporin antibacterial compounds of Formula (!): corresponding pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods for bacterial infections, especially those caused by gram-negative bacteria.

IMPROVED PROCESS FOR THE PREPARATION OF HALO-DIALKOXYBENZENES

The invention describes an improved method for producing halo-dialkoxybenzenes of formula (I) such as 1-fluoro-2, 3-dialkoxybenzene as well as 2-fluoro-1, 4-dialkoxybenzene, Formula (I) by reacting commercial 2-fluorophenol is reacted with an allyl halide

Discovery of a long-acting, peripherally selective inhibitor of catechol- O -methyltransferase

Novel nitrocatechol-substituted heterocycles were designed and evaluated for their ability to inhibit catechol-O-methyltransferase (COMT). Replacement of the pyrazole core of the initial hit 4 with a 1,2,4-oxadiazole ring resulted in a series of compounds endowed with longer duration of COMT inhibition. Incorporation of a pyridine N-oxide residue at position 3 of the 1,2,4-oxadiazole ring led to analogue 37f, which was found to possess activity comparable to entacapone and lower toxicity in comparison to tolcapone. Lead structure 37f was systematically modified in order to improve selectivity and duration of COMT inhibition as well as to minimize toxicity. Oxadiazole 37d (2,5-dichloro-3-(5-(3,4-dihydroxy-5-nitrophenyl)-1,2,4-oxadiazol-3-yl)-4, 6-dimethylpyridine 1-oxide (BIA 9-1067)) was identified as a long-acting, purely peripheral inhibitor, which is currently under clinical evaluation as an adjunct to l-Dopa therapy of Parkinson's disease.

2-IMINOPYRROLIDINE DERIVATES

A 2-iminopyrrolidine derivative represented by the formula: {wherein ring B represents a benzene ring, pyridine ring, etc.; R101 - R103 represent hydrogen, halogen, C1-6 alkyl, etc.; R5 represents hydrogen, C1-6 alkyl, C1-6 alkoxy-C1-6 alkyl, etc.; R6 represents hydrogen, C1-6 alkyl, C1-6 alkyloxycarbonyl, etc.; Y1 represents a single bond, -CH2-, etc.; Y2 represents a single bond, -CO-, etc.; and Ar represents hydrogen, a group represented by the formula: [wherein R10-R14 represent hydrogen, C1-6 alkyl, hydroxyl, C1-6 alkoxy, etc.; and R11 and R12 or R12 and R13 may bond together to form a 5- to 8-membered heterocyclic ring], etc.}, or a salt thereof.

Preparation process of fluorine substituted aromatic compound

A preparation process of a fluorine substituted aromatic compound comprising reacting an alkali metal or alkali earth metal salt of an aromatic compound having a hydroxy group with an organic fluorinating agent is disclosed. As a representative fluorinating agent, a bis-dialkylamino-difluoromethane compound, for example, 2,2′-difluoro-1,3-dimethylimidazolidine, is exemplified. According to the process, an industrially useful fluorinated aromatic compound, for example, a fluorobenzene, a fluorine substituted benzophenone, a fluorine substituted diarylsulfone can be prepared with ease in economy without specific equipment.

Syntheses of Fluorinated 2-Benzylimidazolines

Perturbation of the electronic properties of the phenyl ring of 2-benzylimidazoline without appreciable steric modification can be achieved by fluorine substitution on the phenyl ring.The effects of such perturbation on biological activity can be evaluated.Syntheses of several fluorinated synthetic intermediates and 2-benzylimidazolines are described.Fluorine coupling of ortho benzylic protons and ortho methoxy protons were found to be 0-1.3 Hz.

CONVENIENT, ONE-STEP SYNTHESES OF 2-FLUOROVERATROLE AND 2-FLUOROVERATRALDEHYDE

Metalated veratraldehyde and veratrole were quenched with perchloryl fluoride to provide one-step syntheses of 2-fluoroveratraldehyde and 2-fluoroveratrole, respectively.Previous syntheses of this precursors to 2-fluorodopamine and 5-fluoronorepinephrine are multi-step processess which involve introduction of fluorine at an early stage.Perchloryl fluoride is a potentially hazardous reagant, and should be used only on an appropriate (millimolar) scale with precautions.