736080-30-1

Upstream product

• 6232-11-7 methyl 4-(aminomethyl)benzoate hydrochloride 
• 4023-02-3 1H-pyrazole-1-carboximidamide hydrochloride 

Downstream Products

• 866000-18-2 4-[(4-pyrazin-2-yl-pyrimidin-2-ylamino)-methyl]-benzoic acid 
• 849235-67-2 methyl 4-(((4-(pyridin-3-yl)pyrimidin-2-yl)amino)methyl)benzoate 
• 1448350-18-2 N-(4-bromo-2-nitrophenyl)-4-({[4-(pyridin-3-yl)pyrimidin-2-yl]amino}methyl)benzamide 
• 1448350-16-0 N-hydroxy-4-({[4-(pyridin-3-yl)pyrimidin-2-yl]amino}methyl)benzamid 
• 849235-68-3 4-(([4-(pyridin-3-yl)pyrimidin-2-yl]amino)methyl)benzoic acid 
• 1448350-07-9 N-(3-aminonaphthalen-2-yl)-4-({[4-(pyridin-3-yl)pyrimidin-2-yl]amino}methyl)benzamide 
• 1448350-17-1 N-(2-nitro-4-phenylphenyl)-4-({[4-(pyridin-3-yl)pyrimidin-2-yl]amino}methyl)benzamide 
• 1448350-08-0 N-(2-amino-4-phenylphenyl)-4-({[4-(pyridin-3-yl)pyrimidin-2-yl]amino}methyl)benzamide 
• 1448350-09-1 N-(2-amino-4-bromophenyl)-4-({[4-(pyridin-3-yl)pyrimidin-2-yl]amino}methyl)benzamide 
• 1448350-10-4 N-(2-amino-4-methoxyphenyl)-4-({[4-(pyridin-3-yl)pyrimidin-2-yl]amino}methyl)benzamide 
• 1448350-11-5 N-(2-amino-4-hydroxyphenyl)-4-({[4-(pyridin-3-yl)pyrimidin-2-yl]amino}methyl)benzamide 
• 1448350-19-3 N-(4-{[(tert-butyldimethylsilyl)oxy]methyl}-2-nitrophenyl)-4-({[4-(pyridin-3-yl)pyrimidin-2-yl]amino}methyl)benzamide 
• 1448350-12-6 N-(2-amino-4-{[(tert-butyldimethylsilyl)oxy]methyl}phenyl)-4-({[4-(pyridin-3-yl)pyrimidin-2-yl]amino}methyl)benzamide 
• 1448350-13-7 N-[2-amino-4-(hydroxymethyl)phenyl]-4-({[4-(pyridin-3-yl)pyrimidin-2-yl]amino}methyl)benzamide 

Relevant academic research and scientific papers

PROCESS FOR THE PREPARATION OF SUBSTITUTED PYRIMIDINES

This invention relates to an improved process of making compounds of Formula (I) and synthetic intermediates thereof. (I) In particular, the invention relates to an improved process to prepare N-(2-aminophenyl)-4- ((pyrimidin-2-ylamino)methyl)benzamides which requires fewer steps, is efficient, can be used on an industrial scale, and results in a final product which is suitable for pharmaceutical use.

Discovery of N-(2-Aminophenyl)-4-[(4-pyridin-3-ylpyrimidin-2-ylamino) methyl]benzamide(MGCD0103), an orally active histone deacetylase inhibitor

The design, synthesis, and biological evaluation of N-(2-aminophenyl)-4- [(4-pyridin-3-ylpyrimidin-2-ylamino)methyl]benzamide 8 (MGCD0103) is described. Compound 8 is an isotype-selective small molecule histone deacetylase (HDAC) inhibitor that selectively inhibits HDACs 1-3 and 11 at submicromolar concentrations in vitro. 8 blocks cancer cell proliferation and induces histone acetylation, p21ciP/waf1 protein expression, cell-cycle arrest, and apoptosis. 8 is orally bioavailable, has significant antitumor activity in vivo, has entered clinical trials, and shows promise as an anticancer drug.

INHIBITORS OF HISTONE DEACETYLASE

The invention relates to a series of compounds useful for inhibiting histone deacetylase (HDAC) enzymatic activity. The invention also provides a method for inhibiting histone descetylase in a cell using said compounds as well as a method for treating cell proliferative diseases and conditions using said HDAC inhibitors. Further, the invention provides pharmaceutical compositions comprising the HDAC inhibiting compounds and a pharmaceutically acceptable carrier.

INHIBITORS OF HISTONE DEACETYLASE

The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.