Total Synthesis of Chlorocyclinone A, a PPAR‑γ Antagonist

The first total synthesis of chlorocyclinone A (<b>1</b>) is regioselectively completed in 28 steps. The key steps are Pd-catalyzed methoxycarbonylation, unprecedented Hauser annulation, Krohn photo-oxidation, and regioselective <i>gem</i>-dichlorination

Total Synthesis of Chlorocyclinone A, a PPAR‑γ Antagonist

The first total synthesis of chlorocyclinone A (<b>1</b>) is regioselectively completed in 28 steps. The key steps are Pd-catalyzed methoxycarbonylation, unprecedented Hauser annulation, Krohn photo-oxidation, and regioselective <i>gem</i>-dichlorination

Ag(I)-Catalyzed Indolization/C3-Functionalization Cascade of 2‑Ethynylanilines via Ring Opening of Donor–Acceptor Cyclopropanes

A AgSbF₆-catalyzed cascade involving the ring opening of donor–acceptor cyclopropanes (DACs) preceded by the cyclization of <i>N</i>-protected 2-ethynylaniline is described. The method discloses a step-economy route to 2,3-disubstituted indole, where a Ag catalyst is found to trigger the cascade by activating both alkyne and DACs. Various functionalities at different ends of both substrates offer rapid access to 2,3-disubstituted indole derivatives in one pot in good to excellent yields. Elaboration of the cascade product to useful intermediates is also depicted

Ni(II)-Catalyzed Highly Stereo- and Regioselective Syntheses of Isoindolinones and Isoquinolinones from <i>in Situ</i> Prepared Aldimines Triggered by Homoallylation/Lactamization Cascade

An efficient route to isoindolinones and isoquinolinones has been achieved via a domino Ni-catalyzed homoallylation/lactamization from <i>in situ</i> prepared imines, derived from <i>o</i>-formyl benzoates and <i>o</i>-formyl arylacetates, with conjugated dienes promoted by diethylzinc. The reaction proceeds smoothly at room temperature for a variety of aldehydes, amines, and dienes. The method involves one C–C and two C–N bond forming events under operationally simple conditions