450357-78-5

Upstream product

• 5446-92-4 2-methoxy-5-nitropyridine 
• 22041-27-6 ethoxycarbonylmethyl-trimethyl-ammonium; iodide 
• 38533-61-8 2-chloro-6-methoxy-3-nitropyridine 
• 1000342-55-1 diethyl 2-(6-methoxy-3-nitropyridin-2-yl)malonate 

Downstream Products

• 1615714-05-0 N-(cyclopropylmethyl)-1-(2,4-dimethylbenzyl)-5-methoxy-1H-pyrrolo[3,2-b]pyridine-3-carboxamide 
• 1615714-16-3 C₂₀H₂₂N₂O₃ 
• 1615714-17-4 C₁₈H₁₈N₂O₃ 

Relevant academic research and scientific papers

TRIAZINE DERIVATIVE HAVING EGFR INHIBITORY ACTIVITY, PREPARATION METHOD THEREFOR AND USE THEREOF

Disclosed are a triazine derivative having EGFR inhibitory activity, a preparation method therefor and use thereof. In particular, disclosed are an EGFR inhibitor having a structure of formula (I), a preparation method therefor, a pharmaceutical composition containing same, use thereof for preparing the EGFR inhibitor, and use thereof in preparing medicaments for treating and/or preventing cancers, tumors or metastatic diseases at least partially related to insertion, deletion or other mutation of EGFR exon 20, and in particular use thereof in preparing medicaments for treating and/or preventing hyperproliferative diseases and diseases inducing cell death disorders. The definition of each substituent of formula (I) is the same as that in the description.

Macrocyclic kinase inhibitor and application thereof

The invention belongs to the technical field of medicines, in particular to a macrocyclic tyrosine kinase inhibitor compound, pharmaceutically acceptable salt, ester and stereoisomer of the macrocyclic tyrosine kinase inhibitor compound. More specifically, the tyrosine kinase is one or more of TRK, ALK and ROS1; the present invention relates to a compound, a pharmaceutically acceptable salt thereof, an ester thereof, a stereoisomer thereof, a pharmaceutical composition and a preparation containing the compound, a method for preparing the compound, the pharmaceutically acceptable salt thereof,the ester thereof, and the stereoisomer thereof, and uses of the compound, the pharmaceutically acceptable salt thereof, the ester thereof, and the stereoisomer thereof.

PHARMACEUTICAL COMPOUNDS

This invention relates to compounds that are agonists of the muscarinic M1 receptor or M1 and M4 receptors and which are useful in the treatment of muscarinic M1 or M1/M4 receptor mediated

Lead optimization of 1,4-azaindoles as antimycobacterial agents

In a previous report, we described the discovery of 1,4-azaindoles, a chemical series with excellent in vitro and in vivo antimycobacterial potency through noncovalent inhibition of decaprenylphosphoryl-β-d-ribose-2′- epimerase (DprE1). Nevertheless, high mouse metabolic turnover and phosphodiesterase 6 (PDE6) off-target activity limited its advancement. Herein, we report lead optimization of this series, culminating in potent, metabolically stable compounds that have a robust pharmacokinetic profile without any PDE6 liability. Furthermore, we demonstrate efficacy for 1,4-azaindoles in a rat chronic TB infection model. We believe that compounds from the 1,4-azaindole series are suitable for in vivo combination and safety studies.

Base-mediated reaction of quaternary ammonium salts with nitroarenes - Their useful functionalization via vicarious nucleophilic substitution (VNS)

Ammonium ylides generated from ammonium salt 1a-e with a base react with derivatives of 3-nitropyridine 2a-c and 2-nitrothiophene (3) to form products of vicarious nucleophilic substitution (VNS) 7, 8, or 9 respectively. The products of VNS 10, 11, or 12 are also produced from the corresponding ammonium salts, a base and 4-chloro-nitrobenzene (4), nitrobenzene (5), or 1-nitronaphthalene (6), respectively. In a few products, an exchange of alkoxy group 7c or substitution of chlorine by alkoxyl 8a,b occured.