4.4 Article

Copper(II)-Catalyzed Synthesis of Pyrimidines from Propargylic Alcohols and Amidine: A Propargylation-Cyclization-Oxidation Tandem Reaction

Journal

SYNLETT
Volume -, Issue 8, Pages 1179-1183

Publisher

GEORG THIEME VERLAG KG
DOI: 10.1055/s-0030-1259954

Keywords

pyrimidine; propargylation; amidine; copper; annulation

Funding

  1. National Natural Science Foundation of China [21072159]
  2. Science & Technology Bureau of Xiamen [3502Z20093007]
  3. NFFTBS [J1030415]

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A new approach to the tandem synthesis of 2,4-disubstituted or 2,4,6-trisubstituted pyrimidines from propargylic alcohols with amidine is described. This reaction is catalyzed by 20 mol% Cu(OTf)(2) to give pyrimidines in moderate to good yields via a propargylation-cyclization-oxidation tandem sequence.

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