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

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

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.

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