Redox-neutral zinc-catalyzed cascade [1,4]-H shift/annulation of diaziridines with donor-acceptor aziridines.

The coupling of diaziridines with donor-acceptor aziridines (DAAs) has been achieved using Zn-catalysis to furnish imidazopyrazole-4,4-dicarboxylates via [1,4]-hydride shift. The use of Zn-catalysis, [1,4]-hydride shift, natural product modification and a late-stage molecular docking study are important practical features.

One-pot C-N/C-C bond formation and oxidation of donor-acceptor cyclopropanes with tetrahydroisoquinolines: access to benzo-fused indolizines.

One-pot C-N/C-C bond formation of donor-acceptor cyclopropanes (DACs) with tetrahydroisoquinolines (THIQs) has been achieved to furnish benzo-fused indolizines. These reactions involve a MgI2-catalyzed ring opening of DACs and oxidative annulation using Mn(OAc)3·2H2O. The substrate scope and functional group diversity are the important practical features.

Expedient C-H allylation of sulfoxonium ylides: merging C-H and C-C/C-het bond activation.

Sulfoxonium ylide chelation-assisted C-H allylation of arenes has been accomplished utilizing strained vinyl carbo/heterocycles as the allyl surrogates via sequential C-H and C-C/het bond activation. Broad substrate scope, Co-catalysis, selectivity, and late-stage drug mutation are the important practical features.

Sc(OTf)3-Catalyzed Domino C-C/C-N Bond Formation of Aziridines with Quinones via Radical Pathway.

Sc(III)-catalyzed domino C-C and C-N bond formation of N-sulfonyl aziridines with quinones has been accomplished to furnish functionalized indolines at a moderate temperature. The umpolung reactivity of aziridines, radical pathway, mild reaction conditions, substrate scope, and coupling of drug molecules in a postsynthetic application are the important practical features.

Redox-Neutral Site-Selective C-H Allylation and Iodolactonization of Benzoic Acids Using Morita-Baylis-Hillman Adducts in Water.

A Ru-catalyzed carboxylate directed C-H allylation and iodolactonization of benzoic acids has been accomplished with Morita-Baylis-Hillman adducts as the coupling partner in environmentally benign water as solvent. The redox-neutral conditions, use of water as a solvent, substrate scope, functional group tolerance, and mutation of natural products and drug molecules are the important practical features.

Cascade C-H Activation/Annulation of Sulfoxonium Ylides with Vinyl Cyclopropanes: Access to Cyclopropane-Fused α-Tetralones.

Rh-catalyzed weak and traceless directing-group-assisted cascade C-H activation and annulation of sulfoxonium ylides with vinyl cyclopropanes as a coupling partner have been accomplished to furnish functionalized cyclopropane-fused tetralones at moderate temperature. The C-C bond formation, cyclopropanation, functional group tolerance, late-stage diversifications of drug molecules, and scale-up are the important practical features.

Directed C8-H allylation of quinoline N-oxides with vinylcyclopropanes via sequential C-H/C-C activation.

The Rh(III)-catalyzed C8-allylation of quinoline N-oxides has been accomplished using vinylcyclopropanes as an allyl source with excellent diastereoselectivity at room temperature. The C-H/C-C activation, substrate scope and natural product mutation are the important practical features.