262368-30-9

Basic information

• Product Name: N-(4-aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide
• Synonyms: N-(4-aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide;N-(4-Aminophenyl)-N,4-dimethyl-1-piperazineacetamide;N-[(4-methyl-piperazin-1-yl)methylcarbonyl]-N-methyl-p-phenylendiamine;-N-methyl-2-(4-methylpiperazin-1-yl);Nintedanib Intermediate 2
• CAS NO: 262368-30-9
• Molecular Formula: C₁₄H₂₂N₄O
• Molecular Weight: 262
• EINECS: 919-251-0
• Product Categories: Intermediate of BIBF-1120 and PKI587
• Mol File: 262368-30-9.mol
• Article Data: 19

Chemical Properties

• Melting Point: 148-150
• Boiling Point: 434.8±40.0 °C(Predicted)
• Appearance: /
• Density: 1.151
• Storage Temp.: Keep in dark place,Inert atmosphere,Room temperature
• Solubility: DMSO (Slightly), Methanol (Slightly)
• PKA: 7.43±0.10(Predicted)
• CAS DataBase Reference: N-(4-aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide(CAS DataBase Reference)
• NIST Chemistry Reference: N-(4-aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide(262368-30-9)
• EPA Substance Registry System: N-(4-aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide(262368-30-9)

Safety Data

• Hazardous Substances Data: 262368-30-9(Hazardous Substances Data)

Usage

Uses

N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide acts as a reagent for the preparation, angiokinase inhibitory, antitumor activity and pharmacokinectic properties of deuterated derivatives of nintedanib.

Upstream product

• 109-01-3 1-methyl-piperazine 
• 79-04-9 chloroacetyl chloride 
• 350-46-9 4-Fluoronitrobenzene 
• 74-89-5 methylamine 
• 100-15-2 N-methyl(p-nitroaniline) 
• 586-78-7 para-nitrophenyl bromide 
• 2653-16-9 2-chloro-N-methyl-N-(4-nitrophenyl)acetamide 
• 1139453-98-7 N-methyl-2-(4-methylpiperazin-1-yl)-N-(4-nitrophenyl)-acetamide 

Downstream Products

• 656247-17-5 nintedanib 
• 1160294-26-7 nintedanib 

Relevant articles and documents

Refining method of amino intermediate

The invention relates to a tefining method of an amino intermediate represented by formula (I). Through the refining method, the concentrations of a genotoxic impurity 1 (N-(4-nitrophenyl)-N-methyl-2-(4-methylpiperazin-1-yl) acetamide) and an impurity 2 (N-(4-(hydroxyamino) phenyl)-N-methyl-2- (4-methylpiperazin-1-yl) acetamide) can be controlled to 4 ppm or less. According to the present invention, the contents of the genotoxic impurity 1 and the genotoxic impurity 2 in the formula (I) are significantly reduced, such that the process guarantee is provided for the industrial preparation of high-quality nintedanib ethanesulfonate, and the medication safety is ensured.

Synthesis of the Kinase Inhibitors Nintedanib, Hesperadin, and Their Analogues Using the Eschenmoser Coupling Reaction

A novel synthetic approach involving an Eschenmoser coupling reaction of substituted 3-bromooxindoles (H, 6-Cl, 6-COOMe, 5-NO2) with two substituted thiobenzanilides in dimethylformamide or acetonitrile was used for the synthesis of eight kinase inhibitor

Preparation method of nintedanib key intermediate

The invention belongs to the technical field of pharmaceutical chemicals, and particularly relates to a preparation method of a nintedanib key intermediate compound II. A compound IV is reduced by adopting a common reaction reagent under the conditions of normal temperature and normal pressure, so that a high-purity compound II can be conveniently obtained. The adopted reaction conditions are mild, high-pressure equipment is avoided, the technical operation is simple, the conditions are mild, the process is safer and more environmentally friendly, and the feasibility of large-scale productionof nintedanib is greatly improved.