1201080-46-7

Upstream product

• 91004-38-5 3-acetamido-4-hydroxybenzoic acid 
• 1571-72-8 3-amino-4-hydroxybenzoic acid 
• 536-25-4 methyl 3-amino-4-hydroxybenzoate 
• 126360-59-6 methyl 3-(N-acetyl)amino-4-hydroxybenzoate 
• 1201080-29-6 5-acetamido-4-ethoxy-2-nitrobenzoic acid 
• 1356916-92-1 3-acetamido-4-ethoxybenzoic acid 
• 1201080-20-7 methyl 3-acetamido-4-ethoxybenzoate 

Downstream Products

• 1201080-09-2 N-(3-cyano-7-ethoxy-4-oxo-1,4-dihydroquinolin-6-yl)acetamide 
• 1201079-16-4 N-[5-(2-cyanoacetyl)-2-ethoxy-4-nitrophenyl]acetamide 
• 1201079-19-7 N-{5-[2-cyano-3-(N,N-dimethylamino)acryloyl]-2-ethoxy-4-nitrophenyl}acetamide 
• 1436405-70-7 5-amino-N-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-4-ethoxy-2-nitrobenzamide 
• 1436405-71-8 N-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-5-(4-(dimethylamino)but-2-enamido)-4-ethoxy-2-nitrobenzamide 
• 1436405-72-9 2-amino-N-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-5-(4-(dimethylamino)but-2-enamido)-4-ethoxybenzamide 
• 1436405-73-0 N-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-4-ethoxy-5-(4-((4-methylpiperazin-1-yl)methyl)benzamido)-2-nitrobenzamide 
• 1436405-74-1 2-amino-N-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-4-ethoxy-5-(4-((4-methylpiperazin-1-yl)methyl)benzamido)benzamide 
• 1436405-75-2 5-amino-N-(3-chloro-4-((3-fluorobenzyl)oxy)phenyl)-4-ethoxy-2-nitrobenzamide 
• 1436405-76-3 N-(3-chloro-4-((3-fluorobenzyl)oxy)phenyl)-5-(4-(dimethylamino)but-2-enamido)-4-ethoxy-2-nitrobenzamide 
• 1436405-77-4 2-amino-N-(3-chloro-4-((3-fluorobenzyl)oxy)phenyl)-5-(4-(dimethylamino)but-2-enamido)-4-ethoxybenzamide 
• 1436405-78-5 N-(3-chloro-4-((3-fluorobenzyl)oxy)phenyl)-4-ethoxy-5-(4-((4-methylpiperazin-1-yl)methyl)benzamido)-2-nitrobenzamide 
• 1436405-79-6 2-amino-N-(3-chloro-4-((3-fluorobenzyl)oxy)phenyl)-4-ethoxy-5-(4-((4-methylpiperazin-1-yl)methyl)benzamido)benzamide 
• 1436405-80-9 5-amino-N-(3-chloro-4-fluorophenyl)-4-ethoxy-2-nitrobenzamide 

Relevant academic research and scientific papers

Design, synthesis and biological evaluation of novel pyrimidine, 3-cyanopyridine and m-amino-N-phenylbenzamide based monocyclic EGFR tyrosine kinase inhibitors

36 new compounds with the typical skeleton of 4-anilino-5-vinyl/ethynyl pyrimidine, 4-anilino-3-cyano-5-vinyl/ethynyl/phenyl pyridine, and m-amino-N-phenylbenzamide, are designed, synthesized and selectively tested on EGFR, ErbB-2 kinases, and A-549, HL60 cells growth inhibition. Results from the bioactivity and chemical structures yield preliminary structure-activity relationships (SARs). The most potent 5-ethynylpyrimidine derivative 20a has an IC50 value of 45 nM to EGFR kinase. Several compounds of other series also show IC50 values 1 μM for EGFR and 5 μM for A-549 and HL60 cells growth inhibition.

Synthesis of n-(3-cyano-7-ethoxy-1,4-dihydro-4-oxoquinolin-6-yl)acetamide

New route for the preparation of N-(3-cyano-7-ethoxy-1,4-dihydro-4- oxoquinolin-6-yl)acetamide (1), a key intermediate for the synthesis of selective EGFR kinase inhibitors, was described.