4.8 Article

Pd-Catalyzed Tandem Cyclization of Ethyl Glyoxalate and Amines: Rapid Assembly of Highly Substituted Cyclic Dehydro-α-Amino Acid Derivatives

Journal

ORGANIC LETTERS
Volume 14, Issue 22, Pages 5640-5643

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/ol302483f

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Funding

  1. NCET [10-0371]
  2. NSFC [21072063]
  3. SRF for ROCS [2010-1174]
  4. RFDP [20100172120020]
  5. GNSF [10351064101000000]

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A novel cascade cyclization of ethyl glyoxalate and amines proceeds in the presence of Pd(TFA)(2) (5 mol %) to give the cyclic dehydro-a-amino acid derivatives. This method provides a fast and simple access to highly substituted dihydro-pyrrol-2-ones in good yields.

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