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A novel approach to 3-methylindoles by a Heck/cyclization/isomerization process.

Carl A Baxter1, Ed Cleator, Mahbub Alam

  • 1Department of Process Research, Merck Sharp and Dohme Research Laboratories, Hertford Road, Hoddesdon, Hertfordshire, EN11 9BU, United Kingdom. carl_baxter2@merck.com

Organic Letters
|January 16, 2010
PubMed
Summary

A new three-step method synthesizes 3-methylindoles from chlorotriflates. This efficient Heck reaction, carbamate/aryl chloride coupling, and isomerization sequence allows for quick, regiocontrolled indole synthesis.

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