e.g. Filippa Pettersson or Cancer Res. 75(6) , 1102-12, (2015) or 10.1002/anie.201600521
1, 3-Diaza-1, 3-butadienes. Synthesis and Conversion into Pyrimidines by [4π+ 2π] Cycloaddition with Electron Deficient Acetylenes. Synthetic Utility of 2-( …
Methods have been devised to generate 1 H-1, 3-diaza-1, 3-butadienes bearing a leaving group at position-4 in latent, masked, and unprotected forms. A hallmark of these azadienes is that they undergo thermal [4π+ 2π] cycloaddition reactions with electron deficient acetylenes to give adducts which are aromatized to pyrimidine derivatives under the reaction conditions. Thus, 1-(methoxycarbonyl)-3-acylamidines 17 on heating in solution ...