The diverse reactivity of homopropargylic amines as the "masked" 1C synthons for the aza-Friedel-Crafts alkylation of indoles

A novel type of "masked" 1C synthons was developed through the hydroamination cyclization-protonation of homopropargylic amines to act as aza-Friedel-Crafts alkylation reagents to react with indoles. And a variety of 3-(2-pyrrolidinyl)indoles were generated in good to high yields. More significantly, some of these corresponding products display potential bioactivity for the anti-chlamydial infection, which specifically target the mid-stage of the chlamydial life cycle by interfering with RB replication.

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