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A process for the preparation 2,5-dichloro-N-(2-(isopropylsulfonyl)phenyl)pyrimidin-4- amine

IP.com Disclosure Number: IPCOM000244568D
Publication Date: 2015-Dec-22
Document File: 1 page(s) / 7K

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The IP.com Prior Art Database

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A process for the preparation 2,5-dichloro-N-(2-(isopropylsulfonyl)phenyl)pyrimidin-4- amine

    Provided herein is a process for preparing 2,5-dichloro-N-(2- (isopropylsulfonyl)phenyl)pyrimidin-4-amine, referred to as Compound 3. The process comprises coupling reaction between 2-(isopropylsulfonyl)aniline and 2,4,5- trichloropyrimidine in the presence of the base (e.g. Sodium tert-butoxide, Potassium tert- butoxide, Lithium tert-butoxide, Lithium tert-amoxide) and Lewis acid (e.g. MgCl2, MgBr2, CuCl, CuCl2, SnCl2, ZnCl2, ZnBr2, LiCl, LiOAc, BCl3).

    Compound 3 may be converted to 5-chloro-N2-[2-isopropoxy-5-methyl-4-(4- piperidinyl)phenyl]-N4-[2-(isopropylsulfonyl)phenyl]-2,4-pyrimidinediamine. The conversion may be done according to processes described in the literature, for example, according to the process described in US8039479.