1356962-90-7

Basic information

• Product Name: 1-(1-(5-methoxy-2-methyl-4-nitrophenyl)piperidin-4-yl)-4-methylpiperazine
• Synonyms: 1-(1-(5-methoxy-2-methyl-4-nitrophenyl)piperidin-4-yl)-4-methylpiperazine
• CAS NO: 1356962-90-7
• Molecular Weight: 348.445
• Mol File: 1356962-90-7.mol
• Article Data: 4

Chemical Properties

• CAS DataBase Reference: 1-(1-(5-methoxy-2-methyl-4-nitrophenyl)piperidin-4-yl)-4-methylpiperazine(CAS DataBase Reference)
• NIST Chemistry Reference: 1-(1-(5-methoxy-2-methyl-4-nitrophenyl)piperidin-4-yl)-4-methylpiperazine(1356962-90-7)
• EPA Substance Registry System: 1-(1-(5-methoxy-2-methyl-4-nitrophenyl)piperidin-4-yl)-4-methylpiperazine(1356962-90-7)

Safety Data

• Hazardous Substances Data: 1356962-90-7(Hazardous Substances Data)

Upstream product

• 106579-00-4 5-methoxy-2-methyl-4-nitroaniline 
• 53617-36-0 1-methyl-4-(piperidin-4-yl)piperazine 
• 314298-13-0 1-fluoro-5-methoxy-2-methyl-4-nitro-benzene 
• 109-01-3 1-methyl-piperazine 
• 1356963-00-2 1-(5-methoxy-2-methyl-4-nitrophenyl)piperidin-4-one 
• 452-78-8 3-fluoro-4-methyl phenol 
• 83341-28-0 5-fluoro-4-methyl-2-nitrophenol 
• 1356962-93-0 8-(5-Methoxy-2-methyl-4-nitrophenyl)-1,4-dioxa-8-azaspiro[4.5]decane 

Downstream Products

• 1356963-01-3 2-methoxy-5-methyl-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)aniline 

Relevant articles and documents

Conformational Constrained 4-(1-Sulfonyl-3-indol)yl-2-phenylaminopyrimidine Derivatives as New Fourth-Generation Epidermal Growth Factor Receptor Inhibitors Targeting T790M/C797S Mutations

Tertiary C797S mutation of epidermal growth factor receptor (EGFR)-mediated resistance in non-small-cell-lung-cancer (NSCLC) patients is still an unmet clinical need. Several classes of adenosine 5′-triphosphate-competitive or allosteric EGFRT790M/C797Sinhibitors and degraders have been developed, but none of them have received approval from the regulatory agencies. Herein, we report the structure-based design of conformational constrained 4-(1-ethylsufonyl-3-indolyl)-2-phenylaminopyrimidines as new EGFRT790M/C797Sinhibitors by using a macrocyclization strategy. Representative compound 18j potently inhibited EGFR19del/T790M/C797Sand EGFRL858R/T790M/C797Smutants with IC50values of 15.8 and 23.6 nM and suppressed Ba/F3-EGFRL858R/T790M/C797Sand Ba/F3-EGFR19del/T790M/C797Scells with IC50values of 0.036 and 0.052 μM, respectively, which is 10-20-fold more potent than brigatinib. 18j also potently inhibited the EGFR19del/T790M/C797S-mutated PC-9-OR NSCLC cell proliferation with an IC50value of 0.644 μM but was less potent for parental Ba/F3 and A431 cells. This study provides a new lead compound for drug discovery to combat EGFRC797S-mediated resistance in NSCLC patients.

ARYL-PHOSPHORUS-OXYGEN COMPOUND AS EGFR KINASE INHIBITOR

Disclosed is a class of new aryl-phosphorus-oxygen compounds as shown in formula (I) as EGFR kinase inhibitors, and pharmaceutically acceptable salts thereof.