697762-39-3

Usage

Ethyl ester of 2-(2,4-difluoro-5-iodobenzoyl)-3-diMethylaMinoacrylic acid

2-(2,4-difluoro-5-iodobenzoyl)-3-diMethylaMinoacrylic acid ethyl ester is derived from 2-(2,4-difluoro-5-iodobenzoyl)-3-diMethylaMinoacrylic acid by attaching an ethyl ester group.

Usage as a reagent in organic synthesis

It is commonly used as a reagent in organic synthesis due to its versatile structure and functional groups.

Building block for pharmaceuticals and agrochemicals

The presence of a carboxylic acid, an amino group, and a fluorinated benzoyl group makes it a valuable building block for the preparation of various pharmaceuticals and agrochemicals.

Unique reactivity from fluorine and iodine substituents

The presence of fluorine and iodine atoms on the benzoyl ring provides unique reactivity and potentially useful properties for the compound in various applications.

Easier handling and manipulation in laboratory settings

The ethyl ester group allows for easier handling and manipulation of the compound in laboratory settings.

Upstream product

• 412319-88-1 ethyl-3,3-dimethylaminoacrylate 
• 161531-51-7 2,4-difluoro-5-iodobenzoic acid 
• 1583-58-0 2,4-difluoro-benzoic acid 
• 924-99-2 ethyl 3-(dimethylamino)acrylate 

Downstream Products

• 697762-60-0 7-fluoro-1-(1(S)-hydroxymethyl-2-methylprop-1-yl)-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxylic acid ethyl ester 
• 697762-59-7 C₁₇H₂₀F₂INO₄ 
• 1261283-91-3 6-(3-chloro-2-fluorobenzyl)-7-fluoro-1-[2-methyl-1-(tetrahydropyran-2-yloxymethyl)prop-1-yl]-4-oxo-1,4-dihydroquinoline-3-carboxylic acid ethyl ester 
• 1261283-94-6 6-(3-chloro-2-fluorobenzyl)-7-fluoro-1-((S)-1-hydroxymethyl-2-methylprop-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid dicyclohexylamine salt 
• 1261283-95-7 1(S)-[1-(tert-butyldimethylsilanyloxymethyl)-2-methylprop-1-yl]-6-(3-chloro-2-fluorobenzyl)-7-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 
• 1261283-97-9 6-(3-chloro-2-fluorobenzyl)-7-fluoro-1-[2-methyl-1-(tetrahydropyran-2-yloxymethyl)prop-1-yl]-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 
• 1261283-99-1 1-(S)-[1-(tert-butyldimethylsilanyloxymethyl)-2-methylprop-1-yl]-6-(3-chloro-2-fluorobenzyl)-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 
• 1261284-01-8 6-(3-chloro-2-fluorobenzyl)-7-methoxy-1-[1-(S)-2-methyl-1-(tetrahydropyran-2-yloxymethyl)prop-1-yl]-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 
• 697762-66-6 6-(3-chloro-2-fluorobenzyl)-7-fluoro-1-[1-(S)-tert-butyldimethylsilyloxymethyl-2-methylprop-1-yl]-4-oxo-1,4-dihydroquinoline-3-carboxylic acid ethyl ester 
• 697761-98-1 elvitegravir 
• 869893-92-5 6-(3-chloro-2-fluorobenzyl)-7-fluoro-1-((S)-1-hydroxymethyl-2-methylprop-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 
• 870294-02-3 1-((2S)-1-tert-butyldimethylsilyloxy-3-methylbutan-2-yl)-7-fluoro-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxylic acid ethyl ester 

Relevant academic research and scientific papers

A quinolone derivatives containing pyrimidine ring and its preparation and use

The invention belongs to the technical field of medicines and in particular relates to pyrimidine ring-containing quinolone derivatives as well as a preparation method and application thereof. A compound comprises pyrimidine ring-containing quinolone deri

AN IMPROVED PROCESS FOR THE PREPARATION OF ELVITEGRAVIR

The present invention relates to improved process for the preparation of elvitegravir (12), wherein the compound of formula (6) is protected with suitable protecting agents and further reacted with formula (9) in the presence of tetrakis(triphenylphosphin

HETEROCYCLIC UREA DERIVATIVES AND METHODS OF USE THEREOF

Compounds of formula (IA) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.

Quinolone carboxylic acids as a novel monoketo acid class of human immunodeficiency virus type 1 integrase inhibitors

Human immunodeficiency virus type 1 (HIV-1) integrase is a crucial target for antiretroviral drugs, and several keto - enol acid class (often referred to as diketo acid class) inhibitors have clinically exhibited-marked antiretroviral activity. Here, we show the synthesis and the detailed structure - activity relationship of the quinolone carboxylic acids as a novel monoketo acid class of integrase inhibitors. 6-(3-Chloro-2-fluorobenzyl)-1-((2S)-1-hydroxy-3,3- dimethylbutan-2-yl)-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 51, which showed an IC50 of 5.8 nMin the strand transfer assay and an ED50 of 0.6 nMin the antiviral assay, and 6-(3-chloro-2-fluorobenzyl) -1-((2S)-1-hydroxy-3-methylbutan-2-yl)-7-methoxy-4-oxo-1,4-dihydroquinoline-3- carboxylic acid 49, which had an IC50 of 7.2 nMand an ED50 of 0.9 nM, were the most potent compounds in this class. The monoketo acid 49 was much more potent at inhibiting integrasecatalyzed strand transfer processes than 3′-processing reactions, as is the case with the keto - enol acids. Elvitegravir 49 was chosen as a candidate for further studies and is currently in phase 3 clinical trials.

6- (Heterocyclyl-substituted Benzyl) -4-Oxoquinoline Compound and Use Thereof as HIV Integrase Inhibitor

The present invention relates to a compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, or a solvate thereof, and a pharmaceutical composition, an anti-HIV

4-OXOQUINOLINE COMPOUNDS AND UTILIZATION THEREOF AS HIV INTEGRASE INHIBITORS

An anti-HIV agent containing, as an active ingredient, a 4-oxoquinoline compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof. The compound of the present invention has HIV integrase inhibitory action and is useful as an anti-HIV agent for the prophylaxis or therapy of AIDS. Moreover, by a combined use with other anti-HIV agents such as protease inhibitors, reverse transcriptase inhibitors and the like, the compound can become a more effective anti-HIV agent. Since the compound has high inhibitory activity specific for integrases, it can provide a safe pharmaceutical agent with a fewer side effects for human.

NOVEL 4-OXOQUINOLINE COMPOUND AND USE THEREOF AS HIV INTEGRASE INHIBITOR

Provision of a compound having an anti-HIV activity, particularly an integrase inhibitory activity.A 4-oxoquinoline compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof: wherein each symbol is as defined in the specification.The present invention also relates to a pharmaceutical composition containing the 4-oxoquinoline compound or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier; an integrase inhibitor, an antiviral agent, anti-HIV agent and the like, which contains the 4-oxoquinoline compound or a pharmaceutically acceptable salt thereof as an active ingredient; an anti-HIV composition containing the 4-oxoquinoline compound or a pharmaceutically acceptable salt thereof, and one or more other kinds of anti-HIV activity substances as active ingredients; an anti-HIV agent containing the 4-oxoquinoline compound or a pharmaceutically acceptable salt thereof as an active ingredient, which is used for a multiple drug therapy with other anti-HIV agent(s), and the like.

STABLE CRYSTAL OF 4-OXOQUINOLINE COMPOUND

The present invention provides a crystal of 6-(3-chloro-2-fluorobenzyl)-1-[(S)-1-hydroxymethyl-2-methylpropyl]-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid, which shows a particular powder X-ray diffraction pattern of a characteristic diffractio