Preparation of 3-alkylated indoles

C - Chemistry – Metallurgy – 07 – D

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C07D 209/24 (2006.01) C07C 53/21 (2006.01) C07C 53/50 (2006.01) C07C 205/61 (2006.01) C07C 211/15 (2006.01) C07D 209/08 (2006.01) C07D 209/18 (2006.01)

Patent

CA 2056065

A process for the preparation of a 3-alkylated indole, which comprises:- a) reacting a N-(2-nitrostyryl) enamine with an alkylating agent to afford an imine salt, b) optionally reacting the imine salt with water to afford a (2-nitrophenyl)acetaldehyde, and c) reacting the imine salt or the (2-nitrophenyl)acetaldehyde with a reducing agent capable of selectively reducing the nitro group, to afford the desired 3-alkylated indole.

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