Organic Letters p. 2270 - 2273 (2010)
Update date:2022-08-04
Topics:
Ramanjulu, Joshi M.
Demartino, Michael P.
Lan, Yunfeng
Marquis, Robert
A novel, one-step method for the synthesis of tri- and tetrasubstituted pyrimidin-4-ones is reported. This method involves a titanium(IV)-mediated cyclization involving two sequential condensations of primary and β-ketoamides. The reaction is operationally facile, readily scalable, and offers rapid entry into differentially substituted pyrimidin-4-one scaffolds. The high functional group compatibility allows for substantial diversification in the products generated from this transformation.
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