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A Process for the preparation of N‐(3‐((2‐((4‐(4‐acetylpiperazin‐1‐yl)‐2‐methoxyphenyl)amino)‐5‐ (trifluoromethyl)pyrimidin‐4‐yl)amino)phenyl)acrylamide

IP.com Disclosure Number: IPCOM000244606D
Publication Date: 2015-Dec-28
Document File: 1 page(s) / 110K

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A Process for the preparation of N‐(3‐((2‐((4‐(4‐acetylpiperazin‐1‐yl)‐2‐methoxyphenyl)amino)‐5‐

(trifluoromethyl)pyrimidin‐4‐yl)amino)phenyl)acrylamide 

     Provided herein is a process for preparing  N‐(3‐((2‐((4‐(4‐acetylpiperazin‐1‐yl)‐2‐ methoxyphenyl)amino)‐5‐(trifluoromethyl)pyrimidin‐4‐yl)amino)phenyl)acrylamide, referred herin as  Compound B. The process comprises combining 1‐(4‐(4‐((4‐chloro‐5‐(trifluoromethyl)pyrimidin‐2‐ yl)amino)‐3‐methoxyphenyl)piperazin‐1‐yl)ethanone (either in base or salt form), referred herein as  Compound A, with N‐(3‐aminophenyl)acrylamide, and optionally catalytic amount of acid in an  alcoholic solvent). The process may be done according to any of the processes described for example  in Cancer Discov. 3 (2013) 1404‐1415, Chin. J. Pharm. 45 (2014) 710‐713 or WO 2012/061,299).  

     Compund A in a base or salt form , used as a starting material in the above process, was  preparred by a process comprising  combining 1‐(4‐(4‐Amino‐3‐methoxyphenyl)piperazin‐1‐ yl)ethanone, reffered herein as Compound 1, in base or salt form with 2,4‐dichloro‐5‐ (trifluoromethyl)pyrimidine, using Lewis acid in non‐polar solvents, such as etheric solvents or in  mixtures  of non‐polar solvents with tertiary alcohol...