1351374-48-5

Basic information

• Product Name: N-Cyclopropyl-2-methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzamide
• Synonyms: N-Cyclopropyl-2-methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzamide;N-cyclopropyl-2-methyl-4-(tetramethyl-1,3,2-dioxaborolan-2-yl)benzamide
• CAS NO: 1351374-48-5
• Molecular Weight: 301.193
• Mol File: 1351374-48-5.mol
• Article Data: 17

Chemical Properties

• CAS DataBase Reference: N-Cyclopropyl-2-methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzamide(CAS DataBase Reference)
• NIST Chemistry Reference: N-Cyclopropyl-2-methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzamide(1351374-48-5)
• EPA Substance Registry System: N-Cyclopropyl-2-methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzamide(1351374-48-5)

Safety Data

• Hazardous Substances Data: 1351374-48-5(Hazardous Substances Data)

Upstream product

• 21900-45-8 4-bromo-2-methylbenzoyl chloride 
• 68837-59-2 4-bromo-2-methylbenzoic acid 
• 345965-99-3 4-bromo-N-cyclopropyl-2-methylbenzamide 
• 73183-34-3 bis(pinacol)diborane 

Downstream Products

• 1365243-78-2 [4-(cyclopropylcarbamoyl)-3-methylphenyl]boronic acid 
• 1401449-61-3 4-(4-amino-6-bromo-1H-benzimidazol-1-yl)-N-cyclopropyl-2-methylbenzamide 
• 1401449-62-4 4-{6-bromo-4-[(3,3,3-trifluoropropyl)amino]-1H-benzimidazol-1-yl}-N-cyclopropyl-2-methylbenzamide 
• 1401449-66-8 N-cyclopropyl-2-methyl-4-{6-(pyridin-4-yl)-4-[(3,3,3-trifluoropropyl)amino]-1H-benzimidazol-1-yl}benzamide 
• 1401449-67-9 N-cyclopropyl-4-{6-[(5-fluoro-2-methylphenyl)amino]-4-[(3,3,3-trifluoropropyl)amino]-1H-benzimidazol-1-yl}-2-methylbenzamide 
• 1401449-68-0 N-cyclopropyl-4-{6-(3-fluorophenoxy)-4-[(3,3,3-trifluoropropyl)amino]-1H-benzimidazol-1-yl}-2-methylbenzamide 
• 1401449-81-7 N-cyclopropyl-4-{6-(2,3-difluorophenoxy)-4-[(3,3,3-trifluoropropyl)amino]-1H-benzimidazol-1-yl}-2-methylbenzamide 
• 1402593-77-4 N-cyclopropyl-4-{6-(3-fluoro-4-methoxyphenoxy)-8-[(3,3,3-trifluoropropyl)amino]imidazo[1,2-a]pyridin-3-yl}-2-methylbenzamid 
• 1402594-63-1 N-cyclopropyl-4-{6-(3-fluoro-4-hydroxyphenoxy)-8-[(3,3,3-trifluoropropyl)amino]imidazo[1,2-a]pyridin-3-yl}-2-methylbenzamide 
• 1402595-17-8 4-{6-bromo-8-[(3,3,3-trifluoropropyl)amino]imidazo[1,2-a]pyridin-3-yl}-N-cyclopropyl-2-methylbenzamide 
• 1402594-95-9 N-cyclopropyl-4-{8-[(2,2-difluoroethyl)amino]-6-(3-fluorophenoxy)imidazo[1,2-a]pyridin-3-yl}-2-methylbenzamide 
• 1402596-15-9 tert-butyl {3-[4-(cyclopropylcarbamoyl)-3-methylphenyl]-6-(3-fluorophenoxy)imidazo[1,2-a]pyridin-8-yl}(2,2-difluoroethyl)carbamate 
• 1402596-16-0 tert-butyl {6-bromo-3-[4-(cyclopropylcarbamoyl)-3-methylphenyl]imidazo[1,2-a]pyridin-8-yl}(2,2-difluoroethyl)carbamate 
• 1402593-27-4 N-cyclopropyl-4-{6-[2-(hydroxymethyl)phenyl]-8-[(3,3,3-trifluoropropyl)amino]imidazo[1,2-a]pyridin-3-yl}-2-methylbenzamide 

Relevant articles and documents

Discovery of Pyrazolo[1,5-a]pyrimidine TTK Inhibitors: CFI-402257 is a Potent, Selective, Bioavailable Anticancer Agent

This work describes a scaffold hopping exercise that begins with known imidazo[1,2-a]pyrazines, briefly explores pyrazolo[1,5-a][1,3,5]triazines, and ultimately yields pyrazolo[1,5-a]pyrimidines as a novel class of potent TTK inhibitors. An X-ray structure of a representative compound is consistent with 11/2 type inhibition and provides structural insight to aid subsequent optimization of in vitro activity and physicochemical and pharmacokinetic properties. Incorporation of polar moieties in the hydrophobic and solvent accessible regions modulates physicochemical properties while maintaining potency. Compounds with enhanced oral exposure were identified for xenograft studies. The work culminates in the identification of a potent (TTK Ki = 0.1 nM), highly selective, orally bioavailable anticancer agent (CFI-402257) for IND enabling studies.

PYRAZOLOPYRIMIDINE COMPOUNDS

The present teachings provide a compound represented by the following structural formula: (Formula (I)); or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof.

SUBSTITUTED IMIDAZOPYRIDAZINES

The present invention relates to substituted imidazopyridazine compounds, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.