1429497-82-4

Basic information

• Product Name: ethyl 4-((3-((tert-butoxycarbonyl)amino)phenyl)amino)-2-chloropyrimidine-5-carboxylate
• Synonyms: ethyl 4-((3-((tert-butoxycarbonyl)amino)phenyl)amino)-2-chloropyrimidine-5-carboxylate
• CAS NO: 1429497-82-4
• Molecular Weight: 392.842
• Mol File: 1429497-82-4.mol
• Article Data: 4

Chemical Properties

• CAS DataBase Reference: ethyl 4-((3-((tert-butoxycarbonyl)amino)phenyl)amino)-2-chloropyrimidine-5-carboxylate(CAS DataBase Reference)
• NIST Chemistry Reference: ethyl 4-((3-((tert-butoxycarbonyl)amino)phenyl)amino)-2-chloropyrimidine-5-carboxylate(1429497-82-4)
• EPA Substance Registry System: ethyl 4-((3-((tert-butoxycarbonyl)amino)phenyl)amino)-2-chloropyrimidine-5-carboxylate(1429497-82-4)

Safety Data

• Hazardous Substances Data: 1429497-82-4(Hazardous Substances Data)

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 108-45-2 m-phenylenediamine 
• 51940-64-8 ethyl 2,4-dichloropyrimidine-5-carboxylate 
• 68621-88-5 (3-aminophenyl)carbamic acid tert-butyl ester 

Downstream Products

• 1449424-02-5 12-(3-aminophenyl)-2-((2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)benzo[4,5]imidazo[1,2-a]pyrimido[4,5-d]pyrimidin-5(12H)-one 
• 1449423-87-3 N-(3-(2-((2-methoxy-4-(4-methyl-1-piperazinyl)phenyl)amino)-5-oxobenzo[4,5]imidazo[1,2-a]pyrimido[4,5-d]pyrimidine-12(5H)-yl)phenyl)acrylamide 
• 1449423-89-5 N-(3-(2-((2-methoxy-4-morpholinophenyl)amino)-5-oxoimidazo[1,2-a]pyrimido[4,5-d]pyrimidin-10(5H)-yl)phenyl)acrylamide 
• 1449423-90-8 N-(3-(2-((4-(4-(dimethylamino)piperidin-1-yl)-2-methoxyphenyl)amino)-5-oxoimidazo[1,2-a]pyrimido[4,5-d]pyrimidin-10(5H)-yl)phenyl)acrylamide 
• 1449423-91-9 N-(3-(2-((2-ethoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)-5-oxoimidazo[1,2-a]pyrimido[4,5-d]pyrimidin-10(5H)-yl)phenyl)acrylamide 
• 1449423-81-7 4-((3-((tert-butoxycarbonyl)amino)phenyl)amino)-2-chloropyrimidine-5-carboxylic acid 
• 1449423-92-0 C₂₅H₂₄N₁₀O₄ 
• 1449423-93-1 C₂₆H₂₆N₁₀O₄ 
• 1449423-94-2 C₂₇H₃₁N₉O₂ 
• 1449423-95-3 C₂₈H₃₃N₉O₂ 
• 1449423-82-8 (3-(2-((3-dihydro-[1,2,3]triazolo[4,5-b] pyridine-3-yl)oxy)-5-oxo-7,8-dihydro-imidazo[1,2-a]pyrimido[4,5-d]pyrimidine-10(5H)-yl)phenyl)carbamic acid t-butyl ester 
• 1449423-96-4 C₂₄H₂₀N₁₀O₄ 
• 1449423-83-9 10-(3-amino-phenyl)-2-((2-methoxy-4-(4-methyl-1-piperazinyl)phenyl)amino)-7,8-dihydroimidazo[1,2-a]pyrimido[4,5-d]pyrimidin-5(10H)-one 
• 1449423-97-5 C₂₆H₂₇N₉O₂ 

Relevant articles and documents

Design, Synthesis, and Biological Evaluation of Pyrimido[4,5- d]pyrimidine-2,4(1 H,3 H)-diones as Potent and Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors against L858R/T790M Resistance Mutation

First-generation epidermal growth factor receptor (EGFR) inhibitors, gefitinib and erlotinib, have achieved initially marked clinical efficacy for nonsmall cell lung cancer (NSCLC) patients with EGFR activating mutations. However, their clinical benefit was limited by the emergence of acquired resistance mutations. In most cases (approximately 60%), the resistance was caused by the secondary EGFR T790M gatekeeper mutation. Thus, it is still desirable to develop novel third-generation EGFR inhibitors to overcome T790M mutation while sparing wild-type (WT) EGFR. Herein, a series of pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione derivatives were designed and synthesized, among which the most potent compound 20g not only demonstrated significant inhibitory activity and selectivity for EGFRL858R/T790M and H1975 cells in vitro but also displayed outstanding antitumor efficiency in H1975 xenograft mouse model. The encouraging mutant-selective results at both in vitro and in vivo levels suggested that 20g might be used as a promising lead compound for further structural optimization as potent and selective EGFRL858R/T790M inhibitors.

Pyrimidine and tricyclic or pyrimidine and tetracyclic compound and its medicinal composition and use

The invention discloses pyrimidotricyclic compounds or pyrimidotetracyclic compounds having a structure represented by the formula (I), (II) or (III), pharmaceutically-acceptable salts, stereoisomers, or prodrug molecules. The compounds can inhibit various tumor cells, and especially, the compounds can selectively act on lung cancer cells of EGFR L858R/T790 and EGFR E745 A750/T790M. Compared to wild type cancer cells, the IC50 of the compounds is 10 times, 100 times or even 1000 times higher. The compounds are a novel protein kinase inhibitor, which can overcome the drug resistance of EGFR-TKI and has selectivity.