231278-08-3

Usage

Chemical Structure

Consists of a benzene ring substituted with:
Amino group ( \textNH2 )
Fluoro group ( \textF )
Iodo group ( \textI )

Potential Applications

Pharmaceutical Industry:
May exhibit biological activity
Used in the synthesis of various pharmaceuticals
Chemical Synthesis:
Valuable building block due to fluoro and iodo groups
Enables construction of more complex organic molecules

Intermediate in Organic Synthesis

Importance:
Facilitates the synthesis of other organic compounds
Utility:
Key role in the development of new drugs and materials

Upstream product

• 446-32-2 4-fluoroanthranilic acid 

Relevant academic research and scientific papers

QUINAZOLINE DERIVATIVES USEFUL AS SELECTIVE HDAC6 INHIBITORS

Provided herein is a compound of Formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compo

Synthesis method of 2-bromo-5-cyano-4-fluoromethyl benzoate

The invention belongs to the technical field of drug intermediates, and particularly relates to a synthesis method of 2-bromo-5-cyano-4-fluoromethyl benzoate. The synthesis method of 2-bromo-5-cyano-4-fluoromethyl benzoate is provided for the first time,

An alternative synthesis of the non-small cell lung carcinoma drug afatinib

Afatinib (BIBW2992) is the anticancer drug developed by Boehringer Ingelheim. This work is reporting the synthesis of the afatinib using a new route by Ullmann-Goldberg reaction from corresponding 4-anilinoquinazoline iodide as the last step in the synthesis. This route was not described previously and it could be used for synthesis of afatinib analogues.

Quinazoline derivative and preparation method and application thereof

The invention relates to a quinazoline derivative and a preparation method and application thereof, and belongs to the technical field of medicinal chemistry. The structure of the quinazoline derivative is as shown in a formula I. The quinazoline derivative or a pharmaceutically acceptable salt thereof has an irreversible inhibition effect on tyrosine kinase, the compound can inhibit two kinds of tyrosine kinase of EGFR and HER2 simultaneously, and the compound has good inhibitory activity on multiple cancer cell lines. Please see the formula I in the description.

Bicyclic heteroaromatic compounds as protein tyrosine kinase inhibitors

A pharmaceutical formulation comprising the compound of formula

Quinazolin-4-one derivatives as selective histone deacetylase-6 inhibitors for the treatment of Alzheimer's disease

Novel quinazolin-4-one derivatives containing a hydroxamic acid moiety were designed and synthesized. All compounds were subjected to histone deacetylase (HDAC) enzymatic assays to identify selective HDAC6 inhibitors with nanomolar IC50 values. (E)-3-(2-Ethyl-7-fluoro-4-oxo-3-phenethyl-3,4- dihydroquinazolin-6-yl)-N-hydroxyacrylamide, 4b, is the most potent HDAC6 inhibitor (IC50, 8 nM). In vitro, these compounds induced neurite outgrowth accompanied by growth-associated protein 43 expression, and they enhanced the synaptic activities of PC12 and SH-SY5Y neuronal cells without producing toxic or mitogenic effects. Several of the compounds dramatically increased nonhistone protein acetylation, specifically of α-tubulin. Some of the more potent HDAC6 inhibitors decreased zinc-mediated β-amyloid aggregation in vitro. N-Hydroxy-3-(2-methyl-4-oxo-3-phenethyl-3,4-dihydro- quinazolin-7-yl)-acrylamide, 3f, the most promising drug candidate, selectively inhibits HDAC6 (IC50, 29 nM), practically does not affect human ether-a-go-go-related membrane channel activity (IC50 >10 μM) or cytochrome P450 activity (IC50 >6.5 μM) in vitro, and significantly improves learning-based performances of mice with β-amyloid-induced hippocampal lesions.

HISTONE DEACETYLASES (HDACS) INHIBITORS

Histone deacetylases inhibitors (HDACIs) and compositions comprising the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit are also disclosed.

Anilinoquinazolines as protein tyrosine kinase inhibitors

Heteroaromatic compounds are described, methods for their preparation, pharmaceutical compositions containing them, methods of use, and their use in medicines. In particular, the invention relates to quinazoline and pyridopyrimidine derivatives which exhibit protein tyrosine kinase inhibition.

Anilinoquinazaolines as protein tyrosine kianse inhibitors

Heteroaromatic compounds are described, methods for their preparation, pharmaceutical compositions containing them, methods of use, and their use in medicines. In particular, the invention relates to quinazoline and pyridopyrimidine derivatives which exhibit protein tyrosine kinase inhibition.

BENZIMIDAZOLE QUINOLINONES AND USES THEREOF

Methods of inhibiting various enzymes and treating various conditions are provided that include administering to a subject a compound of Structure I or IB, a pharmaceutically acceptable salt thereof, a tautomer thereof, or a pharmaceutically acceptable salt of the tautomer. Compounds having the Structure I and IB have the following structures and have the variables described herein. Such compounds may be used to prepare medicaments for use in inhibiting various enzymes and for use in treating conditions mediated by such enzymes.