Ad iverses cope of 2-aryl-1,3-dicarbonyl substrates was investigated in an efficient and facile enolate-directed CÀHa lkenylation process using readily availablee lectron-deficient alkenes. The developed domino strategy works under rhodium catalysis, providing ar ange of benzopyran heterocycles by the formationo ft wo distinct CÀCa nd CÀOb onds and one new six-membered ring. The salient features of the protocoli nclude the broad range of previously unexplored 1,3-dicarbonyl substrates for CÀHa lkenylations, good functional group tolerance and rapid assembly of new benzopyrans in generally good to excellent isolated yields. Figure 1. Selected examples of bioactive benzopyrans.[a] Dr.
The title benzopyrans are prepared by a palladium‐catalyzed oxidative annulation/nucleophilic substitution sequence from various dicarbonyl compounds and allylic acetate.
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