20274-69-5

Usage

Uses

Used in Pharmaceutical Industry:
4-Fluoro-3-nitrobenzyl alcohol is used as a reagent for the preparation of EW-7197 (E950000), a highly potent orally bioavailable inhibitor of TGF-β type I receptor kinase. 4-FLUORO-3-NITROBENZYL ALCOHOL 96 is utilized in cancer treatment as an immunotherapeutic or antifibrotic agent, playing a crucial role in modulating the immune response and reducing fibrosis associated with cancer progression.
Used in Chemical Synthesis:
4-Fluoro-3-nitrobenzyl alcohol may be used in the synthesis of 4-fluoro-3-nitrobenzyl chloride, which is another important chemical intermediate with potential applications in various chemical and pharmaceutical processes.

InChI:InChI=1/C7H6FNO3/c8-6-2-1-5(4-10)3-7(6)9(11)12/h1-3,10H,4H2

Upstream product

• 453-71-4 3-nitro-4-fluorobenzoic acid 
• 42564-51-2 4-fluoro-3-nitrobenzaldehyde 
• 1009-35-4 4-fluoro-3-nitrobenzonitrile 
• 459-57-4 4-fluorobenzaldehyde 

Downstream Products

• 115577-35-0 4-fluoro-3-nitrobenzylmethanesufonate ester 
• 173775-54-7 (R)-N-(tert-butoxycarbonyl)-4-fluoro-3-nitrophenylalanine 
• 331731-26-1 (R)-N-(tert-butoxycarbonyl)-4-fluoro-3-nitrophenylalanine methyl ester 
• 178217-05-5 (R)-2-(Benzhydrylidene-amino)-3-(4-fluoro-3-nitro-phenyl)-propionic acid tert-butyl ester 
• 178217-07-7 (R)-[(S)-2-[(R)-2-tert-Butoxycarbonylamino-3-(4-fluoro-3-nitro-phenyl)-propionylamino]-2-(3,5-dimethoxy-phenyl)-acetylamino]-(3-hydroxy-4-methoxy-phenyl)-acetic acid methyl ester 
• 157662-71-0 2-<(3-Hydroxyphenyl)acetamido>-N-(4-fluoro-3-nitrophenethyl)acetamide 
• 157662-72-1 (2R)-2-<(3-Hydroxyphenyl)acetamido>-N-(4-fluoro-3-nitrophenethyl)-p-methoxyphenylacetamide 
• 509094-02-4 (4-cyclohexylamino-3-nitro-phenyl)methanol 
• 42564-51-2 4-fluoro-3-nitrobenzaldehyde 
• 15017-52-4 4-(bromomethyl)-1-fluoro-2-nitrobenzene 
• 1366097-28-0 ((4-fluoro-3-nitrobenzyl)oxy)triisopropylsilane 
• 1330633-52-7 4-fluoro-3-nitrobenzylthioacetic acid 
• 1330633-55-0 4-fluoro-3-nitrobenzylsulfonylacetic acid 
• 1330633-77-6 (E)-2',4',6'-trimethoxystyryl-4-fluoro-3-nitrobenzylsulfone 

Relevant academic research and scientific papers

TYK2 INHIBITORS AND USES THEREOF

Described herein are compounds that are useful in treating a TYK2-mediated disorder. In some embodiments, the TYK2-mediated disorder is an autoimmune disorder, an inflammatory disorder, a proliferative disorder, an endocrine disorder, a neurological disorder, or a disorder associated with transplantation.

Asymmetric Total Synthesis and Evaluation of Antitumor Activity of Ophiorrhisine A and Its Derivatives

The first asymmetric total synthesis of ophiorrhisine A (1), a new cyclic tetrapeptide isolated from Ophiorrhiza nutans, was accomplished via an intramolecular aromatic nucleophilic substitution reaction (IMSNAr) of a linear tripeptide to construct a 14-membered paracyclophane ring, resulting in confirmation of its structure and absolute configuration. The structure-activity relationship study of 1 and its derivatives demonstrated that some derivatives possessed cytotoxicity toward human cancer cell lines A549, HT29, and HCT116.

Heterocycle type derivative and preparing method and pharmaceutical application thereof

The invention relates to a novel heterocycle type derivative, a preparing method thereof, a medicine composition containing the derivative and application of the heterocycle type derivative as therapeutic agent, particularly an FGFR4 inhibitor. The preferable compound has a good inhibiting effect on FGFR4.

Pyrimidine derivatives as well as preparation method and medical applications thereof

The invention relates to pyrimidine derivatives as well as a preparation method and medical applications thereof, in particular to pyrimidine derivatives shown as a general formula (I) in the description, a preparation method and medicinal salts thereof and applications of the pyrimidine derivatives and the medicinal salts as therapeutic agents, especially as FGFR4 (fibroblast growth factor receptor 4) kinase inhibitors. Definitions of substituent groups in the general formula (I) are the same as those in the description.

IMINOTETRAHYDROPYRIMIDINONE DERIVATIVES AS PLASMEPSIN V INHIBITORS

A series of 2-imino-6-methyltetrahydropyrimidin-4(lH)-one derivatives, substituted in the 6-position by a phenyl moiety which in turn is meta-substituted by an optionally substituted unsaturated fused bicyclic ring system containing at least one nitrogen atom, being selective inhibitors of plasmepsin V activity, are beneficial as pharmaceutical agents, especially in the treatment of malaria.

THERAPEUTIC COMPOUNDS

The invention provides compounds of formula (I): wherein, A, C, D, X, and Y have any of the values defined in the specification, and salts thereof. The compounds are SIRT2 inhibitors and are useful for treating SIRT2 associated conditions.

p27 PROTEIN INDUCER

The present invention provides a p27 protein inducing agent comprising a compound represented by general formula (11) below or pharmaceutically acceptable salt thereof as an active ingredient: wherein G 1 , G 2 , G 3 and G 8 are each independently selected from -N= etc., Ring G 6 is selected from divalent aryl etc., A is selected from amino etc., G 4 is selected from oxygen etc., G 5 is selected from oxygen etc., G 7 is selected from -CH 2 - etc., and R 2 is selected from C 1-6 alkyl etc.

Asymmetric synthesis of 3-azide-4-fluoro-L-phenylalanine

The asymmetric synthesis of N-Fmoc-protected 3-azide-4-fluoro-L-phenylalanine as a photoactive phenylalanine analog has been achieved by Sch?llkopf's alkylation.

Discovery of potent, selective, and orally bioavailable inhibitors of interleukin-1 receptor-associate kinase-4

In this Letter, we report the continued optimization of the N-acyl-2-aminobenzimidazole series, focusing in particular on the N-alkyl substituent and 5-position of the benzimidazole based on the binding mode and the early SAR. These efforts led to the discovery of 16, a highly potent, selective, and orally bioavailable inhibitor of IRAK-4.

Microwave-assisted solid-phase synthesis of a 1,2-disubstituted benzimidazole library by using a phosphonium linker

An efficient and rapid microwave-assisted solid-phase method for the synthesis of 5-methyl-1,2-disubstituted benzimidazoles derivatives has been developed. The phosphonium linker, obtained by reaction between polymer-supported triphenylphosphine and 4-fluoro-3-nitrobenzyl iodide, underwent aromatic substitution with primary amines, followed by one-pot reaction with aldehydes in the presence of SnCl2·2H 2O, yielded the benzimidazole system under microwave irradiation. The final products were released from the resin with NaOH under microwave irradiation and were obtained in high purity and good overall yield.