METHOD AND INTERMEDIA USED TO OBTAIN DERIVATIVES OF 1-(1H- BENZIMIDAZOLE-2-IL)-4-(2-AMINOPYRIMIDINE)PIPERIDINE

摘要

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).