1346242-81-6

Basic information

• Product Name: JNJ-42756493
• Synonyms: JNJ-42756493;Erdafitinib;Erdafitinib(JNJ-42756493);N-(3,5-dimethoxyphenyl)-N'-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine;N1-(3,5-Dimethoxyphenyl)-N2-(1-methylethyl)-N1-[3-(1-methyl-1H-pyrazol-4-yl)-6-quinoxalinyl]-1,2-ethanediamine;Suftalan Zine;N-(3,5-Dimethoxyphenyl)-N'-isopropyl-N-[3-(1-methyl-1H-pyrazol-4-yl)-6-quinoxalinyl]-1,2-ethanediamine;N1-(3,5-dimethoxyphenyl)-N2-isopropyl-N1-(3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl)ethane-1,2-diamine
• CAS NO: 1346242-81-6
• Molecular Formula: C₂₅H₃₀N₆O₂
• Molecular Weight: 446.5447
• Product Categories: API
• Mol File: 1346242-81-6.mol

Chemical Properties

• Boiling Point: 662.3±55.0 °C(Predicted)
• Appearance: /
• Density: 1.20±0.1 g/cm3(Predicted)
• Storage Temp.: -20°C Freezer, Under inert atmosphere
• Solubility: DMSO (Slightly), Methanol (Slightly)
• PKA: 9.45±0.29(Predicted)
• CAS DataBase Reference: JNJ-42756493(CAS DataBase Reference)
• NIST Chemistry Reference: JNJ-42756493(1346242-81-6)
• EPA Substance Registry System: JNJ-42756493(1346242-81-6)

Safety Data

• Hazardous Substances Data: 1346242-81-6(Hazardous Substances Data)

Usage

Uses

Used in Pharmaceutical Industry:
JNJ-42756493 is used as a therapeutic agent for [application reason], such as targeting specific biological pathways or modulating cellular processes. Its chemical properties allow it to interact with biopolymers and macromolecules, making it a promising candidate for the development of new drugs and therapies.
Used in Drug Delivery Systems:
JNJ-42756493 is used as a component in the development of novel drug delivery systems, such as organic and metallic nanoparticles. These systems aim to improve the delivery, bioavailability, and therapeutic outcomes of various drugs, including those used in the treatment of cancer and other diseases.

History

In early April of 2019, the US FDA approved Janssen Pharmaceutical Companies' brand name Balversa (erdafitinib) as the first-ever fibroblast growth factor receptor (FGFR) kinase inhibitor indicated for patients with locally advanced or metastatic urothelial carcinoma, with susceptible FGFR3 or FGFR2 genetic alterations, that has progressed during or following platinum-containing chemotherapy, including within 12 months of neoadjuvant or adjuvant platinum-containing chemotherapy. At the same time, the FDA also approved the therascreen FGFR RGQ RT-PCR Kit (Qiagen) for utilization as a companion diagnostic with erdafitinib for selecting patients for the indicated therapy.

Upstream product

• 1346245-10-0 C₂₃H₂₅N₅O₅S 
• 1346133-39-8 N-(3,5-dimethoxyphenyl)-3-(1-methyl-1H-pyrazol-4-yl)-6-quinoxalinamine 
• 58203-30-8 N-(2-chloroethyl)-N-propylamine hydrochloride 
• 1380345-34-5 1-methyl-α-oxo-1H-pyrazole-4-acetaldehyde 
• 875-51-4 4-Bromo-2-nitroaniline 
• 1346245-08-6 N-(3,5-dimethoxyphenyl)-N-[2-[[(1,1-dimethylethyl)dimethylsilyl]oxy]ethyl]-3 -(1-methyl-1H-pyrazol-4-yl)-6-quinoxalinamine 
• 75-31-0 isopropylamine 
• 97-02-9 2,4-Dinitroanilin 
• 706819-66-1 2-bromo-1-(1-methyl-1H-pyrazol-4-yl)ethan-1-one 
• 1083325-87-4 7‐bromo‐2‐(1‐methyl‐1H‐pyrazol‐4‐yl)quinoxaline 
• 2895-21-8 2-chloro-N-isopropylacetamide 

Downstream Products

• 1346245-63-3 C₃₆H₃₉N₇O₄ 
• 1346411-44-6 C₂₈H₃₇N₇O₂ 
• 1346243-60-4 C₃₂H₃₇N₇O₂ 
• 1346253-27-7 C₃₂H₃₅N₇O₄ 

Relevant articles and documents

SOLID STATE FORMS OF ERDAFITINIB SALTS AND PROCESSES FOR PREPARATION OF ERDAFITINIB

The present disclosure relates to solid state forms of Erdafitinib salts, processes for preparation thereof, processes for preparation of Erdafitinib and pharmaceutical compositions thereof.

Method for preparing erdafitinib

The invention provides a method for preparing erdafitinib. According to the method disclosed by the invention, the reaction step number is only four, and the yield of a halogenation reaction product is high. The synthetic route provided by the invention n

Preparation method of 3-(1-methyl-1H-pyrazol-4-yl)-6-quinoxaline amine

The invention discloses a preparation method of erlotinib intermediate 3-(1-methyl-1H-pyrazol-4-yl)-6-quinoxaline amine. According to the preparation method of the invention, 2, 4-dinitroaniline is adopted as an initial raw material, and basic unit reactions such as substitution, reductive cyclization, oxidation, condensation and the like are sequentially carried out to obtain the target intermediate. The preparation process has the advantages of easily available raw materials, rapidness, convenience, economy and environmental protection, is suitable for large-scale production, and provides anew preparation way for industrialization of erlotinib.

Preparation method of 7-bromo-2-(1-methyl-1H-pyrazol-4-yl) quinoxaline

The invention discloses a preparation method of erlotinib intermediate 7-bromo-2-(1-methyl-1H-pyrazol-4-yl). The method comprises the following steps of: 4-bromo-2-nitroaniline is adopted as an initial raw material, and substitution, reductive cyclization, oxidation, condensation and other reactions are sequentially carried out to obtain the target intermediate. The preparation process has the advantages of easily available raw materials, rapidness, convenience, economy and environmental protection, is suitable for large-scale production, and provides a new preparation way for industrialization of erlotinib.

Preparation method of Erdafitinib intermediate

The invention discloses a preparation method of an Erdafitinib intermediate 3-(1-methyl-1H-pyrazole-4-yl)-6-quinoxaline amine. The method comprises the steps of by using 2, 4-dinitroaniline as an initial raw material, sequentially carrying out condensation, reduction, cyclization and other basic unit reactions to obtain the target intermediate. The preparation process has the advantages of easilyavailable raw materials, rapidness, convenience, economy and environmental protection, is suitable for large-scale production, and provides a new preparation way for industrialization of Erdafitinib.

Preparation method of Erdafitinib intermediate

The invention discloses a preparation method of an Erdafitinib intermediate 7-bromo-2-(1-methyl-1H-pyrazole-4-yl) quinoxaline. The method comprises the steps of by using 4-bromo-2-nitroaniline as an initial raw material, sequentially carrying out condensation, reduction, cyclization and other reactions to obtain the target intermediate. The preparation process has the advantages of easily available raw materials, rapidness, convenience, economy and environmental protection, is suitable for large-scale production, and provides a new preparation way for industrialization of Erdafitinib.

Preparation method of 7-bromo-2-(1-methyl-1H-pyrazol-4-yl) quinoxaline

The invention discloses a preparation method of Erdafitinib intermediate 7-bromo-2-(1-methyl-1H-pyrazole-4-yl) quinoxaline. The method comprises the steps of sequentially carrying out substitution, reduction, cyclization and other unit reactions on 4-bromo-2-nitroaniline serving as an initial raw material to obtain the target intermediate. The preparation process has the advantages of easily available raw materials, rapidness, convenience, economy and environmental protection, is suitable for large-scale production, and provides a new preparation way for industrialization of Erdafitinib.

Preparation method of 3-(1-methyl-1H-pyrazol-4-yl)-6-quinoxaline amine

The invention discloses a preparation method of an erdafitinib intermediate 3-(1-methyl-1H-pyrazole-4-yl)-6-quinoxaline amine. The target intermediate is prepared by taking 2,4-dinitroaniline as an initial raw material, and sequentially carrying out basic elementary reaction, such as substitution, reduction, and cyclization. The preparation process has the advantages of easily available raw materials, rapidness, convenience, economy and environmental protection, is suitable for large-scale production, and provides a new preparation way for industrialization of erdafitinib.

PROCESS FOR PREPARATION OF ERDAFITINIB, ITS PURIFICATION AND AMORPHOUS SOLID DISPERSION

An aspect of the present application provides a process for the preparation of Erdafitinib and its pharmaceutically acceptable salts. Another aspect of the present application relates to amorphous solid dispersions of Erdafitinib, process for the preparation thereof and pharmaceutical composition comprising amorphous solid dispersions of Erdafitinib. Another aspect of the present application provides process for purification of Erdafitinib.

PYRAZOLYL QUINAZOLINE KINASE INHIBITORS

The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.