4.8 Article

Microwave-Assisted Solventless Reaction of Iridium-Catalyzed Alkylation of Amines with Alcohols in the Absence of Base

Journal

ORGANIC LETTERS
Volume 13, Issue 19, Pages 5386-5389

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/ol202281h

Keywords

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Funding

  1. National Natural Science Foundation of China [20872026]
  2. Hi-Tech Research and Development Program of China (863 Plan) [2009AA02Z308]
  3. Shanghai Pujiang Talent Plan Project [09PJD008]
  4. National Basic Research Program of China (973 Program) [2010CB912600]
  5. Sino Swiss Science and Technology Cooperation (SSSTC) [EG 30-032010]
  6. Roche R&D Center (China) Ltd.

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Microwave-assisted iridium catalyzed alkylation of amines with alcohols was undertaken under solvent-free and base-free conditions. Such alkylation reactions are green, atom-economic, and effective for mono-, di-, and triaklyation of amines. Good isolated yields were obtained for mono- and dialkylated amines using stoichiometric amounts of amines and alcohols, in the presence of 1 mol % [Cp*IrCl2](2). Reasonable yields of trialkylated products were obtained using 4 equiv of alcohols.

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