221221-13-2

Usage

Chemical compound

Alpha-[(cyclopropylamino)methylene]-2,4-difluoro-3-methoxy-beta-oxo-benzenepropanoic acid ethyl ester

Structure

Complex structure with cyclopropylamino and difluoro groups, as well as a methoxy and beta-oxo functional groups attached to a benzene ring

Derivative

Ethyl ester derivative of a propanoic acid compound

Potential applications

Likely to have potential pharmaceutical applications due to structural similarity to other active pharmaceutical ingredients

Research needs

Further research and testing required to determine specific biological activity and medicinal potential

Upstream product

• 372-18-9 1,3-Difluorobenzene 
• 162101-25-9 2,6-difluorophenylboronic acid 
• 28177-48-2 2,6-difluorophenol 
• 437-82-1 1,3-difluoro-2-methoxybenzene 
• 178974-97-5 2,4-difluoro-3-methoxy-benzoic acid 
• 221221-11-0 2,4-difluoro-3-methoxybenzoyl chloride 
• 16173-58-3 N,N-dimethylaminoacrylic acid ethyl ester 
• 765-30-0 Cyclopropylamine 
• 221221-12-1 ethyl 2,4-difluoro-3-methoxybenzoylacetate 
• 373603-19-1 2,4-difluoro-3-methoxyacetophenone 

Downstream Products

• 221221-15-4 ethyl cyclopropyl-4-oxo-7-fluoro-8-methoxy-1,4-dihydroquinolin-3-carboxylate 

Relevant academic research and scientific papers

1-cyclopropyl-4-oxo-7-fluoro-8-methoxy -1,4-dihydro-quinoline-3-carboxylic acid synthesizing method

The invention discloses a synthesis method of 1-cyclopropyl-4-oxo-7-fluoro-8-methoxy-1,4-dihydroquinolyl-3-carboxylic acid. The synthesis method comprises the following reaction steps: reacting m-difluorophenyl with an organolithium reagent, reacting an obtained aryllithium intermediate with borate, quenching to obtain 2,6-difluorophenylboronic acid and 2,6-difluorophenylborate, reacting 2,6-difluorophenol obtained through oxidation with a methylating reagent, reacting the obtained 2,6-difluorophenylmethyl ether with the organolithium reagent, reacting the obtained corresponding aryllithium intermediate with carbon dioxide, reacting the obtained product with an acylchlorinating reagent to obtain 2,4-difluoro-3-methoxy benzoyl chloride, and performing cyclization, hydrolysis and the like to obtain the 1-cyclopropyl-4-oxo-7-fluoro-8-methoxy-1,4-dihydroquinolyl-3-carboxylic acid. The synthesis method has the advantages as follows: raw materials are easy to obtain; the yield in each step is high; the atom economy is high; the synthesis method is suitable for industrial application.

ANTIBACTERIAL FLUOROQUINOLONE ANALOGS

Compounds having antibacterial activity are disclosed. The compunds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein A, B, D, E, G, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Antimicrobial quinolones, their compositions and uses

This invention relates to novel antimicrobial compounds of formula; wherein X, R1, R3, R5, R6, and R8 are defined in the claims, and to their optical isomers, diastereomers or enantiomers, as well as pharmaceutically-acceptable salts, hydrates, and biohydrolyzable esters, amides and imides thereof, and to compositions and uses of such compounds. The invention also relates to compounds derived from these compounds having antimicrobial uses.