A facile and efficient direct synthesis of N-substituted 4-pyrido[1,2-]pyrimidin-4-imines is developed from α-acyl-β-(2-aminopyridinyl)acrylamides mediated by triflic anhydride (TfO) in the presence of 2-chloropyridine. This amide activation protocol features mild reaction conditions, simple execution, excellent yields, and high chemoselectivity, and is also applied to the synthesis of substituted 4-pyrido[1,2-]pyrimidin-4-ones via a practical one-pot procedure.
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| http://dx.doi.org/10.1021/acs.joc.9b03495 | DOI Listing |
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