4.7 Article

Aluminum Triflate as a Powerful Catalyst for Direct Amination of Alcohols, Including Electron-Withdrawing Group-Substituted Benzhydrols

Journal

ADVANCED SYNTHESIS & CATALYSIS
Volume 354, Issue 13, Pages 2447-2452

Publisher

WILEY-V C H VERLAG GMBH
DOI: 10.1002/adsc.201200536

Keywords

aluminum; amination; benzhydrols; direct substitution; letrozole

Funding

  1. MEXT [2105]
  2. CREST from JST
  3. JSPS
  4. Grants-in-Aid for Scientific Research [22105010, 24106733, 12J05297] Funding Source: KAKEN

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Direct aminations of allylic alcohols, benzylic alcohols, and benzhydrols with electron-withdrawing (F, Br, I, NO2, or CN) substituents were efficiently catalyzed by aluminum triflate [Al(OTf)3] to afford the corresponding biarylamines in high yield, and the dibromo-substituted product was further transformed into letrozole.

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