455-87-8

Usage

InChI:InChI=1/C7H6FNO2/c8-5-3-4(7(10)11)1-2-6(5)9/h1-3H,9H2,(H,10,11)

Upstream product

• 326-67-0 N-(2-fluoro-4-methylphenyl)acetamide 
• 403-21-4 3-fluoro-4-nitrobenzoic acid 
• 7439-89-6 iron 
• 63069-50-1 4-cyano-2-fluoroaniline 
• 352-70-5 m-Fluorotoluene 
• 446-34-4 2-fluoro-4-methyl-1-nitrobenzene 
• 713-11-1 4-acetamido-3-fluorobenzoic acid 

Downstream Products

• 1001346-74-2 4-amino-3-fluoro-N-[(1S,5R)-9-methyl-9-azabicyclo[3.3.1]non-7-yI]benzamide 
• 1137211-17-6 4-(9'-cyclopentyl-5'-methyl-6'-oxo-5',6',8',9'-tetrahydrospiro[cyclopropane-1,7'-pyrimido[4,5-b][1,4]diazepine]-2'-ylamino)-3-fluorobenzoic acid 
• 1137213-46-7 4-(9'-cyclopentyl-5'-methyl-6'-oxo-5',6',8',9'-tetrahydrospiro[cyclobutane-1,7'-pyrimido[4,5-b][1,4]diazepine]-2'-ylamino)-3-fluorobenzoic acid 
• 1137870-06-4 4-(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-ylamino)-3-fluoro-benzoic acid 
• 825-98-9 4-iodo-3-fluorobenzoic acid 
• 103842-00-8 N-(2-fluoro-4-hydroxyphenyl)acetamide 

Relevant academic research and scientific papers

Preparation method of 4-amino-3-fluorobenzoic acid

The invention relates to a preparation method of 4-amino-3-fluorobenzoic acid, which is characterized in that 4-amino-3-fluorobenzoic acid is prepared by taking 3,4-difluorobenzonitrile as a raw material, and perferably, the preparation method comprises the following steps: (1) allowing 3,4-difluorobenzonitrile to react with ammonia to form an intermediate, 3-fluorine-4-aminobenzonitrile, and (2)allowing the intermediate, 3-fluorine-4-aminobenzonitrile, to give a hydrolysis reaction under an alkaline condition to form 4-amino-3-fluorobenzoic acid. The preparation method takes cheap 3,4-difluorobenzonitrile as a main raw material, synthesizes 4-amino-3-fluorobenzoic acid with high yield and high purity through steps of ammoniation and hydrolysis, has the advantages of convenience in operation, low price and low environmental pollution, and can achieve large-scale industrial production.

Gas-liquid flow hydrogenation of nitroarenes: Efficient access to a pharmaceutically relevant pyrrolobenzo[1,4]diazepine scaffold

Using a Tube-in-Tube device based on the amorphous Teflon AF-2400 fluoropolymer, a series of nitroarenes was hydrogenated to afford the corresponding aniline compounds. The system was then applied to the construction of a pyrrolobenzo[1,4]diazapene scaffold through a tandem hydrogenation-condensation-hydrogenation sequence.

Substituted 3-fluorophenyl methanol compound, pharmaceutical composition and application

The invention relates to a substituted 3-fluorophenyl methanol compound, a pharmaceutical composition and application in the field of chemical pharmacy. The invention relates to the substituted 3-fluorophenyl methanol compound. Compared with valganciclovir and ganciclovir, the effectiveness of the compound is obviously strengthened, the safety performance is greatly improved, the selectivity index is obviously improved, and huge application value is achieved. The invention further discloses application of the substituted 3-fluorophenyl methanol compound serving as an antiviral drug, and specially for application in preparing a drug for preventing and treating cytomegaloviruses. The invention further discloses a pharmaceutical composition containing the compound and application in preparing the drug for treating or preventing the cytomegalovirus infection disease by utilizing the substituted 3-fluorophenyl methanol compound or the pharmaceutical composition thereof.

Design and synthesis of peptide conjugates of phosphoramide mustard as prodrugs activated by prostate-specific antigen

A series of Glutaryl-Hyp-Ala-Ser-Chg-Gln-4-aminobenzyl phosphoramide mustard conjugates (1a-e) was designed and synthesized as potential prodrugs for site-specific activation by PSA in prostate cancer cells. All conjugates were found to be substrates of PSA with cleavage occurring between Gln and the para-aminobenzyl (PAB) linker. Structure-activity relationship studies on these conjugates indicated that introduction of electron-withdrawing fluorine(s) on the phenyl ring in the PAB linker uniformly improved the chemical stability of the conjugates while the position of substitution affected differently the self-immolative process of conjugates upon proteolysis. Introduction of a fluorine at ortho position to benzylic phosphoramide as in 1b results in better stability of the conjugate prior to activation while maintaining its antiproliferative activity upon activation by PSA. The conjugate 1b with 2-fluoro substitution was identified as a promising lead for further evaluation and optimization in the development of prostate cancer-targeted prodrugs.

Pyrrolidinyl and pyrrolinyl ethylamine compounds as kappa agonists

A compound of the following formula: and the salts thereof wherein A is hydrogen, halo, or hydroxy, broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1is optionally substituted phenyl; Ar2is aryl or heteroaryl selected from phenyl, napththyl, or pyridyl, the aryl or heteroaryl being optionally substituted; R1is hydrogen, hydroxy, or C1-C4alkyl; and R2and R3are independently selected from optionally substituted C1-C7alkyl, C3-C6cycloalkyl, C2-C6alkenyl, C2-C6alkynyl, or R2and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine. These compounds are useful as kappa agonists.