Macrocycles are essential in protein‐protein interactions and the preferential intake of
bioactive scaffolds. Macrocycles are commonly synthesized by late‐stage …

Here, we report a novel strategy for constructing maleimide-containing peptides and cyclic
peptides using Rh (III)-catalyzed tryptophan (Trp)(C7) alkenylation, which is challenging due …

Transition metal-catalyzed aromatic functionalization reactions are highly important for the
construction of various organic fine chemicals. In particular, the direct C (sp2)-H bond …

We describe an Ir‐catalyzed intramolecular reaction of 2‐alkynyl diaryl sulfides, which gives
9‐arylidene‐9H‐thioxanthene derivatives via 6‐exo‐dig cyclization. When 2‐alkynylphenyl …

Heterocycle-braced cyclic peptides have demonstrated enhanced metabolic stability,
increased potency and selectivity. Here, we present a rapid synthesis method for …

A Ru (II)-catalyzed skeletal editing of oxindole scaffolds was established to afford C7-alkyl
acetate indole derivatives using internal alkyne and alkyl alcohol. The developed method is …

The C3‐alkenylation of indoles have been developed by means of a novel in situ iodination
tactic which is capable of mediating the Heck coupling with alkenes. The method features …

Indole derivatives are fundamental structural units in many bioactive compounds and
molecular materials. The site‐selective C7‐functionalization of these moieties has been …

A process for the synthesis of C7-functionalized indoles using para-substituted 2-
alkynylanilines as starting materials was reported. The process involves a dearomatization …

Abstract Strategic direct C─ H functionalization of heterocycles is a cutting-edge approach
for crafting and modifying diverse bio-relevant molecules featuring heterocyclic frameworks …