1345336-53-9

Upstream product

• 915711-42-1 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-aminobenzamide 
• 420-04-2 CYANAMID 
• 96-98-0 4-methyl-3-nitrobenzoic acid 
• 10397-30-5 4-methyl-3-nitrobenzoyl chloride 
• 1449570-25-5 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-nitrobenzamide hydrochloride 
• 2458-12-0 3-amino-p-toluic acid 
• 41191-92-8 3-amino-4-methylbenzoic acid ethyl ester 
• 330807-44-8 3-((tert-butoxycarbonyl)amino)-4-methylbenzoic acid methyl ester 
• 18595-18-1 3-amino-4-methyl benzoic acid methyl ester 

Downstream Products

• 641571-10-0 nilotinib 
• 923288-95-3 Nilotinib hydrochloride 

Relevant academic research and scientific papers

Preparation method and intermediate of nilotinib

The invention discloses a nilotinib preparation method and an intermediate of nilotinib. The preparation method comprises: in a solvent, carrying out a reaction defined in the specification on a compound D or a hydrochloride salt thereof, and a compound SM3 under the action of an inorganic base to obtain the compound E nilotinib. According to the present invention, the preparation method has characteristics of simple reaction, easy operation, safe and environmentally friendly reagent, less side reaction and short reaction time. The reaction formula is defined in the specification.

PROCESS FOR THE PREPARATION OF NILOTINIB

The present invention relates a process for the preparation of a compound of formula (I): or a pharmaceutically acceptable salt thereof, which process comprises converting a compound of formula (IV): or a pharmaceutically acceptable salt thereof, into the compound of formula (I) or a pharmaceutically acceptable salt thereof.

Research and development of a novel process for nilotinib: A Bcr-Abl inhibitor

In this study, an efficient, economic and novel process for the production of highly pure nilotinib (1), a Bcr-Abl inhibitor in described. The synthesis comprises the chlorination of 4-methyl-3-nitro benzoic acid (2) to get 4-methyl-3-nitro benzoyl chloride (2A). Condensation of compound (2) with 5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)-benzeneamine (11) to obtain 4-methyl-N-[3-(4-methyl-1Himidazol- 1-yl-5-(trifluoromethyl)phenyl]-3-nitro- benzamide hydrochloride (3). Reducing compound (3) with stannous chloride (or) raney nickel to obtain 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl-5- (trifluoromethyl)phenyl]-3-amino-benzamide (4). Reaction of compound (4) with cyanamide to obtain 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl-5-(trifluoromethyl) phenyl]-3-guanidino-benzamide (5). Condensation of the compound (5) with 3-dimethylamino-1-(3-pyridyl)-2-propen-1-one (8) to obtain nilotinib (1).

Process for the preparation of nilotinib hydrochloride

A process for the preparation of a hydrochloride salt of a compound of formula (I): which process comprises converting a compound of formula (IV): or a pharmaceutically acceptable salt thereof, into the hydrochloride salt of the compound of formula (I).