Process for the preparation of nmda antagonists

C - Chemistry – Metallurgy – 07 – C

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C07C 231/02 (2006.01) C07C 237/06 (2006.01)

Patent

CA 2273286

This invention relates to an improved process for the production of known amine compounds of formula (I) which are useful as medicaments, wherein: R1 and R2 are independently phenyl or 4-fluorophenyl; R3 is hydrogen, alkyl C1-4 or methoxycarbonyl; R4 is hydrogen or methyl; which comprises reaction of a compound of formula (II) with a compound of formula (III) in which R5, R6, R7, R8, R9 and R10 are independently C1-6 alkyl followed by deprotection and optionally thereafter forming a pharmaceutically acceptable salt.

Cette invention concerne un procédé amélioré permettant de produire des composés amine connus qui sont utilisés comme médicaments et qui correspondent à la formule (I) où R?1¿ et R?2¿ représentent indépendamment phényle ou 4-fluorophényle, tandis que R?3¿ représente hydrogène, alkyle C¿1-4? ou méthoxycarbonyle, et que R?4¿ représente hydrogène ou méthyle. Ce procédé consiste à faire réagir un composé correspondant à la formule (II) avec un composé correspondant à la formule (III) où R?5¿, R?6¿, R?7¿, R?8¿, R?9¿ et R?10¿ représentent indépendamment alkyle C¿1-6?. Ce procédé consiste ensuite à effectuer une déprotection, puis à préparer éventuellement un sel de ces composés acceptable sur le plan pharmaceutique.

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