JNJ-42756493

Base Information

• Chemical Name: JNJ-42756493
• CAS No.: 1346242-81-6
• Molecular Formula: C25H30N6O2
• Molecular Weight: 446.552
• Mol file: 1346242-81-6.mol

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

Chemical Property of JNJ-42756493

Chemical Property:

• Boiling Point: 662.3±55.0 °C(Predicted)
• PKA: 9.45±0.29(Predicted)
• PSA: 77.33000
• Density: 1.20±0.1 g/cm3(Predicted)
• LogP: 4.57450
• Storage Temp.: -20°C Freezer, Under inert atmosphere
• Solubility.: DMSO (Slightly), Methanol (Slightly)

Purity/Quality:

98% ^*data from raw suppliers

Erdafitinib ^*data from reagent suppliers

Safty Information:

• Pictogram(s):  
• Hazard Codes: 

MSDS Files:

SDS file from LookChem

Useful:

• Description: Erdafitinib is an oral pan-FGFR (1-4) inhibitor with has demonstrated promising activity in patients with metastatic or unresectable UC and other histologies (eg, cholangiocarcinoma) with FGFR alterations. It is used in the therapy of locally advanced, unresectable or metastatic urothelial carcinoma. Erdafitinib has been associated with a high rate of serum enzyme elevations during therapy, but has not been linked to cases of clinically apparent acute liver injury.
• Uses: Erdafitinib is a fibroblast growth factor receptor inhibitor.

Technology Process of JNJ-42756493

There total 36 articles about JNJ-42756493 which guide to synthetic route it. The literature collected by LookChem mainly comes from the sharing of users and the free literature resources found by Internet computing technology. We keep the original model of the professional version of literature to make it easier and faster for users to retrieve and use. At the same time, we analyze and calculate the most feasible synthesis route with the highest yield for your reference as below:

synthetic route:

Reference yield: 91.0%

C25H30N6O2*(x)ClH → N1-(3,5-dimethoxyphenyl)-N2-(1-methylethyl)-N1-[3-(1-methyl-1H-pyrazol-4-yl)-6-quinoxalinyl]-1,2-ethanediamine (1346242-81-6)

Guidance literature:

With ammonium hydroxide; In dichloromethane; water; pH=9.5; Product distribution / selectivity;

Reference yield: 89.7%

N-(3,5-dimethoxyphenyl)-N-[2-[[(1,1-dimethylethyl)dimethylsilyl]oxy]ethyl]-3 -(1-methyl-1H-pyrazol-4-yl)-6-quinoxalinamine (1346245-08-6) + isopropylamine (75-31-0) → N1-(3,5-dimethoxyphenyl)-N2-(1-methylethyl)-N1-[3-(1-methyl-1H-pyrazol-4-yl)-6-quinoxalinyl]-1,2-ethanediamine (1346242-81-6)

Guidance literature:

N-(3,5-dimethoxyphenyl)-N-[2-[[(1,1-dimethylethyl)dimethylsilyl]oxy]ethyl]-3 -(1-methyl-1H-pyrazol-4-yl)-6-quinoxalinamine; With methanesulfonyl chloride; triethylamine; In dichloromethane; at 20 ℃; for 4h; Inert atmosphere;

isopropylamine; In acetonitrile; at 100 ℃; for 18h;

Reference yield: 86.5%

C23H25N5O5S (1346245-10-0) + isopropylamine (75-31-0) → N1-(3,5-dimethoxyphenyl)-N2-(1-methylethyl)-N1-[3-(1-methyl-1H-pyrazol-4-yl)-6-quinoxalinyl]-1,2-ethanediamine (1346242-81-6)

Guidance literature:

In acetonitrile; at 100 ℃; for 18h; Product distribution / selectivity; sealed vessel;

upstream raw materials:

3.5-dimethoxyaniline

C₂₃H₂₅N₅O₅S

isopropylamine

7-bromo-2-chloroquinoxaline

Downstream raw materials:

C₃₆H₃₉N₇O₄

C₃₂H₃₅N₇O₄

C₂₈H₃₇N₇O₂

C₃₂H₃₇N₇O₂

Refernces

• 1、 -. "Method for preparing erdafitinib". . . Retrieved 2021/06/26.
• 2、 -. "Preparation method of Erdafitinib intermediate". Paragraph 0034-0035. . Retrieved 2020/12/31.