Abstract
AbstractChemoselective approaches were developed for derivatizing diastereoselective chromanone spiro‐γ‐lactams through the Michael‐type addition by using amide as a weak nucleophile to construct the spiro‐carbon center under basic conditions. To expand the scope of this post‐Ugi cascade reaction, a new series of oxidized chromone derivatives was synthesized by altering solvent from EtOH to DMF. Compounds 7 a and 7 b which could be synthesized in one day, demonstrated comparable anticancer activities with legendary anticancer drug paclitaxel in the PANC and U87 cell lines. This methodology offers a new approach to construct spiro‐carbon centers with functionalized chromanones or chromones under mild reaction conditions.magnified image
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