A synthetic methodology for the reductive alkylation at the...

C - Chemistry – Metallurgy – 07 – D

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C07D 209/18 (2006.01)

Patent

CA 2549120

A process for the reductive alkylation at the C-3 position of an indole compound in which the indole is treated with an aldehyde in the presence of a Lewis acid and a silicon hydride reducing agent. The process is useful for alkylating the C-3 position of indoles that contain acid-sensitive substituents at the N-1 position.

L'invention concerne un processus d'alkylation réductrice à la position C-3 d'un composé d'indole, dans lequel l'indole est traité avec un aldéhyde en présence d'un acide de Lewis et d'un agent réducteur d'hydrure de silicium. Le processus de l'invention est utile pour l'alkylation de la position C-3 d'indoles contenant des substituants sensibles à l'acide à la position N-1.

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