Method and intermedia used to obtain derivatives of...

Details Method and intermedia used to obtain derivatives of... Method and intermedia used to obtain derivatives of...

C - Chemistry, Metallurgy

07

D

C07D 401/04 (2006.01) C07D 211/58 (2006.01) C07D 235/30 (2006.01) C07D 239/42 (2006.01) C07D 401/14 (2006.01)

Patent

CA 2500815

The invention relates to a method of obtaining derivatives of 1-(1H- benzimidazole-2-il)-4-(2-aminopyrimidine)piperidine (IV), wherein R1 represents hydrogen or 4-halobenzyl and R5 represents optionally-substituted hydrogen, alkyl or benzyl. The inventive method comprises the conversion of a 1-[1-(R1)-1H-benzimidazole-2-il]-4-(R2)(R3)-piperidine (I), wherein R2 or R3 represents optionally-protected hydroxy, or R2 and R3 represent, independently of each other, optionally-substituted alkoxy or benzyloxy, or R2 and R3 together form an optionally-substituted alkylenedioxy group, by means of hydrolysis and/or oxidation into a 1-[1-(R1)-1H-benzimidazole-2-il]-4- piperidone, which, by reductive amination (with optional separation of the intermediate imina formed) provides the corresponding amine which, by reaction with a pyrimidine, produces the above-mentioned derivative of 1-(1H- benzimidazole-2-il)-4-(2-aminopyrimidine) piperidine (IV).

L'invention concerne un procédé d'obtention de dérivés de 1-(1H-benzimidazol-2-yl)-4-(2-aminopyrimidine)pipéridine (IV), où R¿1? désigne un hydrogène 4-halobenzile et R¿5? désigne hydrogène, alkyle ou benzyle éventuellement substitués, qui comprend l'étape de conversion d'une 1-[1-(R¿1?)1H-benzimidazol-2-yl]-4-(R¿2?)(R¿3?)-pipéridine (I), où un des R¿2? ou R¿3? désigne hydroxy, éventuellement protégé, ou alors R¿2? et R¿3 ?désignent, de manière indépendante, alcoxy ou benzyloxy éventuellement substitués, ou encore R¿2? et R¿3? forment ensemble un groupe alkylène dioxy, éventuellement substitué, par hydrolyse et/ou par oxydation en une 1-[1-(R¿1?)-1H-benzimidazol-2-yl]-4-pipéridone, qui, par amination réductrice, (avec séparation éventuelle de l'imine intermédiaire formée) fournit l'amine correspondante qui, par réaction avec une pyrimidine, permet l'obtention dudit dérivé de 1-(1H-benzimidazol-2-yl)-4-(2-aminopyrimidine) pipéridine (IV).

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