847502-81-2

Usage

Uses

3,4-Difluoro-2-methylbromobenzene

InChI:InChI=1/C7H5BrF2/c1-4-5(8)2-3-6(9)7(4)10/h2-3H,1H3

Upstream product

• 3828-49-7 1,2-difluoro-3-methyl-benzene 
• 348-61-8 1-bromo-3,4-difluorobenzene 
• 77-78-1 dimethyl sulfate 
• 74-88-4 methyl iodide 

Downstream Products

• 847502-83-4 3,4-difluoro-2-methylbenzonitrile 
• 160775-14-4 3,4-difluoro-2-methylbenzoic acid methyl ester 
• 2136287-65-3 3,4-difluoro-2-((phenylthio)methyl)benzoic acid 
• 2136287-66-4 7,8-difluoro-6,11-dihydrodibenzo[b,e]thiazepin-11-one 
• 1985607-83-7 7,8-difluoro-6,11-dihydrodibenzo[b,e]thiazepine-11-ol 
• 1188413-04-8 C₁₁H₁₄F₂O₃S 
• 1188412-57-8 (1S)-2-(3,4-difluoro-2-methylphenyl)-1-methylethyl azide 
• 157652-31-8 3,4-difluoro-2-methyl benzoic acid 
• 1251164-88-1 3-fluoro-2-methyl-4-(methylsulfonyl)benzoyl chloride 
• 118287-06-2 3-fluoro-2-methyl-4-(thiomethyl)benzoic acid 
• 118939-18-7 3-fluoro-2-methyl-4-(methylsulfonyl)benzoic acid 
• 1251156-08-7 [7-(6-aminopyridin-3-yl)-2,3-dihydro-1,4-benzoxazepin-4(5H)-yl][3-fluoro-2-methyl-4-(methylsulfonyl)-phenyl]methanone 
• 1251150-14-7 C₂₅H₂₂FN₃O₄S 

Relevant academic research and scientific papers

Preparation method of baloxavir intermediate

The invention relates to a preparation method of a baloxavir intermediate and belongs to the field of medicinal chemistry. With the compound (A) as an initial raw material, the method includes a halogenation reaction, a Grignard reaction, a halogenation r

CARBOXAMIDES AS MODULATORS OF SODIUM CHANNELS

Compounds, and pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels are provided. Also provided are pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts and methods of using the compounds, pharmaceutically acceptable salts, and pharmaceutical compositions in the treatment of various disorders, including pain.

Xofluza sulfur-containing heterocyclic compound, intermediate and preparation method thereof

The invention discloses an Xofluza sulfur-containing heterocyclic compound, an intermediate and a preparation method thereof, and provides a preparation method of a compound represented by a formula 5. The preparation method is mild in reaction condition,

Method for preparing baloxavir intermediate and intermediate obtained by method

The invention belongs to the technical field of chemical synthesis, and provides a method for preparing a balosavir intermediate. The method comprises the following steps: (1) methylating 3,4-difluorobromobenzene to obtain a compound A-1; (2) reacting the compound A-1 with a Grignard reagent, then introducing carbon dioxide gas for reaction, and adding acid for acidification to obtain a compound A-2; (3) brominating the compound A-2 to obtain a compound A-3; (4) adding diphenyl disulfide and a reducing agent 1 into THF, dropwise adding methanol, dropwise adding the compound A-3, and reacting to obtain a compound A-4; (5) carrying out ring closing reaction on the compound A-4 in polyphosphoric acid to obtain a compound A-5; and (6) reducing the compound A-5 into alcohol by adopting a reducing agent 2 to obtain a compound A-6. According to the method, highly toxic and foul thiophenol is prevented from being used while expensive reagents are prevented from being used, so that the processcost is reduced. The invention also provides an intermediate compound prepared by the method.

Preparation method of 7,8-difluoro-6,11-dihydro-dibenzothiophene-11-alcohol

The invention relates to a preparation method of 7,8-difluoro-6,11-dihydro-dibenzothiophene-11-alcohol. According to the method, specifically, 2,3-difluorotoluene is adopted as a raw material, and 7,8-difluoro-6,11-dihydro-dibenzothiophene-11-alcohol is e

Process Development and Scale-Up of a Benzoxazepine-Containing Kinase Inhibitor

The benzoxazepine core is present in several kinase inhibitors, including the mTOR inhibitor 1. The process development for a scalable synthesis of 7-bromobenzoxazepine and the telescoped synthesis of 1 are reported. Compound 1 consists of three chemicall

Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR)

A series of novel, highly potent, selective, and ATP-competitive mammalian target of rapamycin (mTOR) inhibitors based on a benzoxazepine scaffold have been identified. Lead optimization resulted in the discovery of inhibitors with low nanomolar activity and greater than 1000-fold selectivity over the closely related PI3K kinases. Compound 28 (XL388) inhibited cellular phosphorylation of mTOR complex 1 (p-p70S6K, pS6, and p-4E-BP1) and mTOR complex 2 (pAKT (S473)) substrates. Furthermore, this compound displayed good pharmacokinetics and oral exposure in multiple species with moderate bioavailability. Oral administration of compound 28 to athymic nude mice implanted with human tumor xenografts afforded significant and dose-dependent antitumor activity.

5,6,7,8-TETRAHYDRO[1,2,4]TRIAZOLO[4,3-a]PYRAZINE DERIVATIVES AS P2X7 MODULATORS

The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein A is hydrogen, C1-4alkyl, C3-6cycloalkyl, C1-3alkoxy, C1-3alkoxy C1-4alkyl, C1-2fluoroalkyl, halogen, NR6 R7, optionally substituted heteroaryl (Het), or optionally substituted phenyl, and R1, R2, R3, R4, R5, R6 and R7 are as defined in the description. The compounds or salts are thought to modulate P2X7 receptor function and to be capable of antagonizing the effects of ATP at the P2X7 receptor. The invention also provides the use of the compound or salt in the treatment or prophylaxis of, for example, inflammatory pain, neuropathic pain, visceral pain, rheumatoid arthritis, osteoarthritis or neurodegenerative disorders.

Difluoroalkylaromatics

The present invention relates to 3,4-difluoro-2-alkylaromatics and 2,4-difluoro-3-alkylaromatics, to a process for their preparation and to their use for preparing active ingredients.