348133-46-0

Usage

Uses

Used in Pharmaceutical Industry:
1,2-Benzenediamine,4-fluoro-N2-methyl-(9CI) is used as a key intermediate in the synthesis of various pharmaceuticals. Its unique structure allows it to be incorporated into a range of drug molecules, enhancing their therapeutic properties and effectiveness.
Used in Organic Compounds Production:
1,2-Benzenediamine,4-fluoro-N2-methyl-(9CI) is also utilized in the production of various organic compounds, contributing to the development of new materials and chemical products with diverse applications.
Used in Medical Research:
1,2-Benzenediamine,4-fluoro-N2-methyl-(9CI) has potential applications in the field of medical research, where it can be employed to study the mechanisms of drug action, develop new therapeutic agents, and improve our understanding of biological processes.
However, it is crucial to handle this chemical with care, as it can be toxic if ingested or inhaled, and may cause skin and eye irritation upon contact. Proper safety measures should be taken to minimize the risks associated with its use.

Upstream product

• 120381-42-2 4-fluoro-2-methylaminonitrobenzene 
• 446-35-5 2,4-Difluoronitrobenzene 

Downstream Products

• 348133-45-9 6-fluoro-1-methyl-1,3-dihydro-2H-benzimidazol-2-one 
• 2050908-30-8 1-(2-chloropyrimidin-4-yl)-5-fluoro-3-methyl-1H-benzo[d]imidazol-2(3H)-one 
• 1191924-08-9 C₂₁H₁₆Cl₂FN₅ 

Relevant academic research and scientific papers

From methylene bridged diindole to carbonyl linked benzimidazoleindole: Development of potent and metabolically stable PCSK9 modulators

Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a recently validated therapeutic target for lowering low-density lipoprotein cholesterol (LDL-C). Through phenotypic screening, we previously discovered a class of small-molecules with a 2,3′-diindolymethane (DIM) skeleton that can decrease the expression of PCSK9. But these compounds have low potency and low metabolically stability. After performing structure-activity relationship (SAR) optimization by nitrogen scan, deuterium substitution and fluorine scan, we identified a series of much more potent and metabolically stable PCSK9 modulators. A preliminary in vivo pharmacokinetic study was performed for representative analogues difluorodiindolyketone (DFDIK) 12 and difluorobenzoimidazolylindolylketone (DFBIIK-1) 13. The in vitro metabolic stability correlate well with the in vivo data. The most potent compound 21 has the EC50 of 0.15 nM. Our SAR studies also indicated that the NH on the indole ring of 21 can tolerate more function groups, which may facilitate the mechanism of action studies and also allow further improvement of the pharmacological properties.

2, 4-DI-(NITROGEN CONTAINING GROUP) SUBSTITUTED PYRIMIDINE COMPOUND AND PREPARATION METHOD AND USE THEREOF

Provided are a 2, 4-di-(nitrogen containing group) substituted pyrimidine compound represented by a general formula (I), a pharmaceutically acceptable salt and a stereoisomer thereof, a preparation method thereof, and a use thereof in preparation of anti-tumor drugs. The compound having a structural feature shown in the general formula (I) can selectively suppress activity of mutant epidermal growth factor receptors (EGFR), including single-mutant EGFR (T790M) and double-mutant EGFR (including L858R/T790M and ex19del/T790M), and can suppress activity of single gain-of-function mutant EGFR (including L858R and ex19del) as well. The compound has a weak suppression effect on wild-type EFGR and a very high selectivity, and thus it has a potential to be used in preparation of drugs for treating EGFR mutant tumors, especially non-small cell lung cancer (NSCLC) comprising a T790M EGFR mutation.

Benzimidazole compound and application thereof

The invention relates to a benzimidazole compound and an application thereof. The structure of the benzimidazole compound is shown as a formula I, and the compound is used as a focal adhesion kinase inhibitor and shows relatively good focal adhesion kinase (FAK) inhibition activity. Meanwhile, the benzimidazole compound has stronger medicine effect and better pharmacokinetic property and/or toxicological characteristics, such as good brain/plasma ratio, good bioavailability, good metabolic stability, and reduced inhibition to respiratory action of mitochondria. The benzimidazole compound has agood clinical application prospect.

PARG INHIBITORY COMPOUNDS

The present invention relates to compounds of formula I that function as inhibitors of PARG (Poly ADP-ribose glycohydrolase) enzyme activity: wherein R1a, R1b, R1c, R1d, R1e, W, X1, X2, X3, X4, X5, X6, X7, c are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which PARG activity is implicated.

TRICYCLIC COMPOUNDS AS TEC KINASE INHIBITORS

The present invention is directed to tricyclic compounds of formula (I) as Tec kinase inhibitors, in particular ITK (interleukin-2 inducible tyrosine kinase) inhibitors. Also provided herein are processes for preparing compounds described herein, intermed

ALDOSTERONE SYNTHASE INHIBITORS

The invention involves compounds of structural Formula (I) and the pharmaceutically acceptable salts thereof. The compounds of the invention are effective at selectively inhibiting CYP11B2, and are therefore useful for the treatment or prophylaxis of disorders that are associated with elevated aldosterone levels, including, but not limited to, hypertension and heart failure.

Linear free energy substitutent effect on flavin redox chemistry

A systematic study on the effect of various substituents at the 7- and/or 8-position on the redox properties of isoalloxazines (flavins) is reported. The redox properties of these flavin derivatives were studied by cyclic voltammetry in 100 mM, pH 7.4 HEPES and 200 mM, pH 10 borate buffers. The magnitude and direction of the effect was dependent on the nature and location of the substituent. The redox potentials of the substituted flavins were correlated with the Hammett σ value of the substituents.