724726-05-0

Usage

Uses

Used in Pharmaceutical Industry:
2-(2-chloropyridin-4-yl)-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4(5H)-one is used as a key intermediate in the synthesis of pyrrolopyridine inhibitors of Mitogen-Activated Protein Kinase-Activated Protein Kinase 2 (MK-2). These inhibitors play a crucial role in regulating cellular processes and have potential therapeutic applications in treating various diseases, including inflammatory and autoimmune disorders.
Used in Cancer Research:
2-(2-chloropyridin-4-yl)-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4(5H)-one is also utilized in the development of heteroaryl-substituted pyrrolopyridinones and their analogs, which act as cdc7 kinase inhibitors. Cdc7 kinase is a promising target for cancer therapy, as it is involved in the regulation of DNA replication and cell cycle progression. Inhibiting this enzyme can lead to the suppression of tumor growth, making these pyrrolopyridinones potential antitumor agents.

Upstream product

• 50607-30-2 piperidine-2,4-dione 
• 23794-15-2 1-(2-chloropyridin-4-yl)ethan-1-one 
• 23794-16-3 2-bromo-1-(2-chloropyridin-4-yl)ethan-1-one 
• 33252-30-1 2-chloro-4-pyridinenitrile 

Relevant academic research and scientific papers

NHC-Copper Mediated Ligand-Directed Radiofluorination of Aryl Halides

[18F]-labeled aryl fluorides are widely used as radiotracers for positron emission tomography (PET) imaging. Aryl halides (ArX) are particularly attractive precursors to these radiotracers, as they are readily available, inexpensive, and stable. However, to date, the direct preparation of [18F]-aryl fluorides from aryl halides remains limited to SNAr reactions between highly activated ArX substrates and K18F. This report describes an aryl halide radiofluorination reaction in which the C(sp2)-18F bond is formed via a copper-mediated pathway. Copper N-heterocyclic carbene complexes serve as mediators for this transformation, using aryl halide substrates with directing groups at the ortho position. This reaction is applied to the radiofluorination of electronically diverse aryl halide derivatives, including the bioactive molecules vismodegib and PH089.

SUBSTITUTED DIHYDRO-1H-PYRROLO[3,2-c]PYRIDIN-4(5H)-ONES AS RIPK3 INHIBITORS

Compounds having Formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, are useful as kinase modulators, including RIPK3 modulation. All the variables defined herein.

Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2)

A new class of potent kinase inhibitors selective for mitogen-activated protein kinase-activated protein kinase 2 (MAPKAP-K2 or MK-2) for the treatment of rheumatoid arthritis has been prepared and evaluated. These inhibitors have IC50 values as low as 10 nM against the target and have good selectivity profiles against a number of kinases including CDK2, ERK, JNK, and p38. These MK-2 inhibitors have been shown to suppress TNFα production in U397 cells and to be efficacious in an acute inflammation model. The structure-activity relationships of this series, the selectivity for MK-2 and their activity in both in vitro and in vivo models are discussed. The observed selectivity is discussed with the aid of an MK-2/inhibitor crystal structure.