What question did this study set out to answer?

The aim is to develop an efficient synthetic approach for indole‐fused eight‐membered heterocycles using rhodium(III) catalysis.

Synthesis of Indole‐Fused Eight‐Membered Heterocycles via Rh( III )‐Catalyzed NH ‐Indole‐Directed C–H Activation/5+3 Annulation of 7‐Phenylindoles with Methyleneoxetanones

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This research unveils efficient synthesis of indole‐fused heterocycles, indicating new methods for drug discovery.

The aim is to develop an efficient synthetic approach for indole‐fused eight‐membered heterocycles using rhodium(III) catalysis.
Utilized rhodium(III) as a catalyst for C–H activation.
Conducted [5+3] annulation using 7‐phenylindoles and methyleneoxetanones.
Employed TsCl/DMAP for intramolecular amidation to form lactams.
Optimized conditions with Cp*RhCl2 catalyst in methanol at 60 °C.
Utilized density functional theory calculations for mechanistic insights.
Achieved good yields for disubstituted acrylic acid intermediates.
Synthesis method expanded the range of accessible non-canonical N-heterocycles.
Demonstrated broad substrate scope with diverse functional groups.
Confirmed key reaction intermediates through isolation and crystallographic analysis.
DFT calculations indicated a favored β‐oxygen elimination pathway.

Lu et al. (2026) studied this question.

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