1190380-50-7

Basic information

• Product Name: 4-Nitro-1-(tetrahydro-2H-pyran-4-yl-1H-pyrazole
• Synonyms: 4-Nitro-1-(tetrahydro-2H-pyran-4-yl-1H-pyrazole;4-nitro-1-(oxan-4-yl)pyrazole
• CAS NO: 1190380-50-7
• Molecular Formula: C8H11N3O3
• Molecular Weight: 197.19124
• Product Categories: Aromatics, Heterocycles, Miscellaneous Reagents
• Mol File: 1190380-50-7.mol
• Article Data: 17

Chemical Properties

• Boiling Point: 365.6±32.0 °C(Predicted)
• Appearance: /
• Density: 1.49±0.1 g/cm3(Predicted)
• PKA: -1.49±0.19(Predicted)
• CAS DataBase Reference: 4-Nitro-1-(tetrahydro-2H-pyran-4-yl-1H-pyrazole(CAS DataBase Reference)
• NIST Chemistry Reference: 4-Nitro-1-(tetrahydro-2H-pyran-4-yl-1H-pyrazole(1190380-50-7)
• EPA Substance Registry System: 4-Nitro-1-(tetrahydro-2H-pyran-4-yl-1H-pyrazole(1190380-50-7)

Safety Data

• Hazardous Substances Data: 1190380-50-7(Hazardous Substances Data)

Usage

Description

4-Nitro-1-(tetrahydro-2H-pyran-4-yl-1H-pyrazole is a chemical compound that serves as a reagent in the synthesis of various pharmaceutical agents.

Uses

Used in Pharmaceutical Synthesis:
4-Nitro-1-(tetrahydro-2H-pyran-4-yl-1H-pyrazole is used as a reagent for the synthesis of LRRK2 modulators, which are important in the treatment of neurodegenerative diseases such as Parkinson's disease. Its unique structure allows for the development of compounds that can modulate the activity of the LRRK2 enzyme, potentially slowing disease progression.
Additionally, 4-Nitro-1-(tetrahydro-2H-pyran-4-yl-1H-pyrazole is used as a reagent in the synthesis of janus kinase inhibitors. These inhibitors are employed in the treatment of various inflammatory and autoimmune diseases by targeting the JAK family of enzymes, which play a crucial role in cell signaling pathways. The use of this reagent contributes to the development of more effective and targeted therapies for these conditions.

Upstream product

• 2075-46-9 4-nitro-1H-pyrazole 
• 134419-59-3 4-oxanyl methanesulfonate 
• 29943-42-8 Tetrahydro-4H-pyran-4-one 
• 25637-16-5 4-bromotetrahydro-2H-pyran 
• 2081-44-9 Tetrahydro-pyran-4-ol 
• 25637-18-7 4-iodotetrahydropyran 
• 19752-88-6 (3RS,4SR)-4-methoxytetrahydropyran 

Downstream Products

• 1202486-35-8 5-(3-(methylsulfonyl)phenyl)-N-(1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-amine 
• 1190380-49-4 1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-amine 

Relevant articles and documents

PYRROLO(PYRAZOLO)PYRIMIDINE DERIVATIVE AS LRRK2 INHIBITOR

The present invention relates to a pyrrolo(pyrazolo)pyrimidine derivative having efficacy as an LRRK2 inhibitor, a preparation method therefor, and a pharmaceutical composition for preventing or treating degenerative brain diseases, containing the same.

TGF-betaR1 inhibitor and application thereof

The invention belongs to the field of medical chemistry, and particularly relates to a compound serving as a TGF-betaR1 inhibitor and application of the compound. Specifically, the invention providesa compound shown as a formula I or an isomer, a pharmaceutically acceptable salt, a solvate, a crystal or a prodrug thereof, a preparation method of the compounds, a pharmaceutical composition containing the compounds and application of the compounds or the composition to treatment and/or prevention of TGF-betaR1 related diseases, such as cancers, tissue hyperplasia diseases, fibrosis and inflammatory diseases. The compound provided by the invention shows significant inhibitory activity on TGF-betaR1 kinase, and is very expected to become a therapeutic agent for TGF-betaR1 related diseases.

Design, synthesis and biological evaluation of novel 7H-pyrrolo[2,3-d]pyrimidine derivatives as potential FAK inhibitors and anticancer agents

A series of 7H-pyrrolo[2,3-d]pyrimidine derivatives possessing a dimethylphosphine oxide moiety were designed, synthesized and evaluated as novel Focal adhesion kinase (FAK) inhibitors. Most compounds potently suppressed the enzymatic activities of FAK, with IC50 values in the 10?8–10?9 M range, and potently inhibited the proliferation of breast (MDA-MB-231) and lung (A549) cancer cell lines. The representative compound 25b exhibited potent enzyme inhibition (IC50 = 5.4 nM) and good selectivity when tested on a panel of 26 kinases. 25b exhibited antiproliferative activity against A549 cells (IC50 = 3.2 μM) and relatively less cytotoxicity to a normal human cell line HK2. Compound 25b also induced apoptosis and suppressed the migration of A549 cells in a concentration-dependent manner. Further profiling of compound 25b revealed it had good metabolic stability in mouse, rat and human liver microsomes in vitro and showed weak inhibitory activity against various subtypes of human cytochrome P450. The docking study of compound 25b was performed to elucidate its possible binding modes and to provide a structural basis for further structure-guided design of FAK inhibitors.