Cascade Reaction to Selectively Synthesize Multifunctional Indole Derivatives by Ir -Catalyzed C-H Activation.

An effective and condition-controlled way to synthesize with high selectivity a variety of functionalized indoles with potent biological properties has been developed. Notably, 2,4-dialkynyl indole products were obtained by direct double C-H bond alkynylation, whereas alkynyl at the C4 position could convert to carbonyl to generate 2-alkynyl-3,4-diacetyl indoles fast and effectively. Additionally, a one-pot relay catalytic reaction led to 2,5-di-alkynyl-3,4-diacetyl indoles when using a carbonyl group as the directing group and by controlling the type and quantity of additives.

Ruthenium-Catalyzed P-Directed Remote ε-C-H Alkylation of Phosphines.

The ruthenium-catalyzed remote ε-C-H alkylation of phosphines with tertiary alkyl halides has been developed. This novel P-directed C-H activation strategy tolerated various functional groups and delivered a wide variety of modified phosphines with excellent site selectivity. Preliminary mechanistic studies indicated that a P-assisted cyclometalation/remote σ-activation pathway might be involved in this methodology.

Iridium(III)-Catalyzed C-H Amidation/Cyclization of -Sulfoximines with -Alkoxyamides: Formation of Thiadiazine 1-Oxides.

The first example of Ir(III)-catalyzed C-H activation/cyclization with -alkoxyamides as amidation reagents to simultaneously form functionalized thiadiazine 1-oxide derivatives was developed. This one-pot cascade protocol tolerated diverse functional groups and readily constructed various heterocyclic frameworks in moderate to good yield.

Synthesis of rhodium(iii)-catalyzed isoquinoline derivatives from allyl carbonates and benzimidates with hydrogen evolution.

A novel Rh(iii)-catalyzed cascade C-H activation/cyclization approach to access isoquinoline derivatives from benzimidates and available allyl carbonates with the liberation of H2 has been realized. Allyl carbonates were first used as a versatile and universal C2 synthon to synthesize this biological activity skeleton via an efficient and practical process just within 1 h.

Specific Synthesis of 3-Indole Derivatives via Rh(III)-Catalyzed Cascade Annulation between -Phenylbenzimidamides and Pyridotriazoles.

An efficient synthetic method to construct -indole derivatives has been successfully developed involving rhodium-catalyzed highly selective C-H bond activation of -phenylbenzimidamides and subsequent couplings with pyridotriazoles. This cascade approach features excellent chemoselectivity and unique of products containing quaternary carbon center with the pyridyl moiety.