1402045-53-7

Upstream product

• 537-92-8 3-Methylacetanilide 
• 67-63-0 isopropyl alcohol 
• 78944-97-5 1-isopropoxy-4-methyl-2-nitrobenzene 
• 108-24-7 acetic anhydride 
• 119-33-5 4-methyl-2-nitrophenol 

Downstream Products

• 1190399-91-7 5-chloro-N²-[2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl]-N⁴-[2-(isopropylsulfonyl)phenyl]pyrimidine-2,4-diamine dihydrochloride 
• 1380575-43-8 5-chloro-N₂-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N₄-(2-(propane-2-sulfonyl)phenyl)pyrimidine-2,4-diamine dihydrochloride 
• 1035230-24-0 5-chloro-N²-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N⁴-((2-isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine 
• 1032900-25-6 5-chloro-N²-{5-methyl-4-(piperidin-4-yl)-2-[(propan-2-yl)oxy]phenyl}-N⁴-[2-(propane-2-sulfonyl)phenyl]pyrimidine-2,4-diamine 

Relevant academic research and scientific papers

PROCESS FOR PREPARATION OF CERITINIB

The present application relates to a process for preparation of ceritinib and intermediates thereof. Specifically, the present application relates to a process for preparation of N-(4-(1-benzyl- 1,2,3,6-tetrahydropyridin-4-yl)-2-isopropoxy-5-methylphenyl)acetamide (VC) comprising treating N-(4-(bromomethyl)-2-isopropoxy-5-methylphenyl)acetamide (IIID) with 1- benzylpiperidin-4-one (IVA). The present application also relates to a process for conversion of N-(4-(1-benzyl-1,2,3,6-tetrahydropyridin-4-yl)-2-isopropoxy-5-methylphenyl)-acetamide (VC) to ceritinib or an acid-addition salt thereof.

Palladium-catalyzed ortho-alkoxylation of anilides via C-H activation

A palladium-catalyzed ortho-alkoxylation of anilides with both primary and secondary alcohols via ligand-directed C-H activation has been explored. This alkoxylation promoted by catalytic methanesulfonic acid proceeds well at room temperature in most cases and affords aryl alkyl ethers in moderate to good yields.