Process for preparing n-methyladamantyl derivatives by a...

C - Chemistry – Metallurgy – 07 – C

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C07C 231/12 (2006.01)

Patent

CA 2662037

The application concerns a process for preparing 2-chloro-5- (3-amino) -N- (methyladamantyl) -benzamide derivatives. The first step of the process involves a palladium catalysed coupling reaction between an iodine containing compound and allyl alcohol with a tertiary amine as base. The second step involves a reductive amination on the formed aldehyde followed by subsequent transformation of the formed amine into a pharmaceutically acceptable salt.

. La présente invention concerne un procédé de préparation de dérivés de 2-chloro-5-(3-amino)-N-(méthyladamantyl)-benzamide. La première étape du procédé comprend une réaction de couplage catalysée au palladium entre un composé iodé cet un alcool d'allyle avec une amine tertiaire comme base. La second étape comprend une amination réductrice sur l'aldéhyde formé suivie d'une transformation ultérieure de l'amine formée en un sel pharmaceutiquement acceptable.

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