Synthesis of β-Keto Esters In-Flow and Rapid Access to Substituted Pyrimidines

Added on:
17 Nov, 2010

We have developed an in-flow process for the synthesis of β-keto esters via the BF3·OEt2-catalyzed formal C−H insertion of ethyl diazoacetate into aldehydes. The β-keto esters were then condensed with a range of amidines to give a variety of 2,6-substituted pyrimidin-4-ols.

  • Hannah E. Bartrum1
  • David C. Blakemore2
  • Christopher J. Moody1
  • Christopher J. Hayes1
  • 1School of Chemistry, University of Nottingham, UK
  • 2Pfizer Global Research and Development, Sandwich, UK
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