945397-01-3

Basic information

• Product Name: 4-chloro-N-(3,5-dimorpholin-4-ylphenyl)pyrimidin-2-amine
• Synonyms: 4-chloro-N-(3,5-dimorpholin-4-ylphenyl)pyrimidin-2-amine
• CAS NO: 945397-01-3
• Molecular Weight: 375.858
• Mol File: 945397-01-3.mol
• Article Data: 5

Chemical Properties

• CAS DataBase Reference: 4-chloro-N-(3,5-dimorpholin-4-ylphenyl)pyrimidin-2-amine(CAS DataBase Reference)
• NIST Chemistry Reference: 4-chloro-N-(3,5-dimorpholin-4-ylphenyl)pyrimidin-2-amine(945397-01-3)
• EPA Substance Registry System: 4-chloro-N-(3,5-dimorpholin-4-ylphenyl)pyrimidin-2-amine(945397-01-3)

Safety Data

• Hazardous Substances Data: 945397-01-3(Hazardous Substances Data)

Upstream product

• 220954-17-6 4,4’-(5-nitro-1,3-phenylene)dimorpholine 
• 2265-94-3 1,3-difluoro-5-nitrobenzene 
• 945397-00-2 N-(3,5-dimorpholin-4-ylphenyl)formamide 
• 97229-11-3 4-chloro-2-methanesulfonylpyrimidine 

Downstream Products

• 1051901-06-4 4-chloro-N-(3,5-dimorpholin-4-ylphenyl)-N-[(4-methoxyphenyl)methyl]pyrimidin-2-amine 
• 1051899-45-6 N-(3,5-dimorpholin-4-ylphenyl)-N'-methyl-pyrimidine-2,4-diamine 
• 1051897-08-5 N-(3,5-dimorpholin-4-ylphenyl)-N'-(3-methoxyphenyl)-N'-methyl-pyrimidine-2,4-diamine 
• 1051897-31-4 N'-(4-chlorophenyl)-N-(3,5-dimorpholin-4-ylphenyl)-N'-methyl-pyrimidine-2,4-diamine 
• 1051898-81-7 N₂-(3,5-dimorpholinophenyl)-N₄-isopropyl-N₄-(3-methoxyphenyl)pyrimidine-2,4-diamine 
• 1051897-42-7 N'-(2,3-difluorophenyl)-N-(3,5-dimorpholin-4-ylphenyl)-N'-methyl-pyrimidine-2,4-diamine 
• 1051899-64-9 N₂-(3,5-dimorpholinophenyl)-N₂-(4-methoxybenzyl)-N₄-(3-methoxyphenyl)pyrimidine-2,4-diamine 
• 1051899-65-0 N₂-(3,5-dimorpholinophenyl)-N₄-isopropyl-N₂-(4-methoxybenzyl)-N₄-(3-methoxyphenyl)pyrimidine-2,4-diamine 
• 1051901-20-2 C₃₂H₃₄F₂N₆O₃ 
• 1051897-23-4 N-(3,5-dimorpholin-4-ylphenyl)-N'-methyl-N'-(2-methylphenyl)pyrimidine-2,4-diamine 
• 1051897-11-0 N-(3,5-dimorpholin-4-ylphenyl)-N'-methyl-N'-phenyl-pyrimidine-2,4-diamine 
• 1051897-32-5 N-(3,5-dimorpholin-4-ylphenyl)-N'-(5-methoxy-2-methyl-phenyl)-N'-methyl-pyrimidine-2,4-diamine 
• 1051897-14-3 N-(3,5-dimorpholin-4-ylphenyl)-N'-methyl-N'-(3-methylphenyl)pyrimidine-2,4-diamine 
• 1051897-10-9 N'-(3-chlorophenyl)-N-(3,5-dimorpholin-4-ylphenyl)-N'-methyl-pyrimidine-2,4-diamine 

Relevant articles and documents

PYRIMIDINE DERIVATIVES

The invention concerns benzamide compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, ring A, n, R3, and R4 are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions which are sensitive to the inhibition of EphB4, and/or EphA2 and/or Src kinases.

Inhibitors of the tyrosine kinase EphB4. Part 3: Identification of non-benzodioxole-based kinase inhibitors

Starting from the initial bis-anilinopyrimidine 1, good potency against EphB4 was retained when benzodioxole at C-4 was replaced by an indazole. The key interactions of the indazole with the protein were characterised by crystallographic studies. Further optimisation led to compound 20, a potent inhibitor of the EphB4 and Src kinases with good pharmacokinetics in various preclinical species and high fraction unbound in plasma. Compound 20 may be used as a tool for evaluating the potential of EphB4 kinase inhibitors in vivo.

NOVEL PYRIMIDINE DERIVATIVES 698

The invention concerns compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, n, R2, R3, and R4 are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions which are sensitive to the inhibition of EphB4 kinases.