An enyne cycloisomerization/[5+1] reaction sequence to synthesize tetrahydroisoquinolinones from enyne-enes and CO.

An enyne cycloisomerization/[5+1] reaction sequence was developed to synthesize tetrahydroisoquinolinones from linear enyne-enes and CO. The first step is a gold(i)-catalyzed enyne cycloisomerization, generating six-membered-ring-fused vinylcyclopropanes. The second step is a rhodium(i)-catalyzed [5+1] reaction of vinylcyclopropanes with CO. This two-step reaction could also be carried out in one-pot without isolating the cycloisomerization product generated from the first step of this sequence.