Yue Huang

A [4 + 1] annulation between newly designed ortho-electrophile-substituted para-quinone methides and nucleophiles through tandem 1,6-conjugated addition/1,4-Michael addition under mild reaction conditions has been described. This reaction provides an efficient method to construct indanes and isoindolines in moderate to good yields and with good functional group tolerance.

A Rh(III)-catalyzed intramolecular olefin hydroarylation of aromatic aldehydes with a transient directing group has been described. The bidentate directing groups in situ generated from aromatic aldehydes and β-alanine could enable the subsequent C–H activation and hydroarylation with excellent site selectivities and high functional group compatibility. The further conversion of the aldehyde group showcased the broad application prospects of this methodology.

A formal 1,6-conjugated addition-mediated [4 + 1] annulation of ortho-hydroxyphenyl-substituted para-quinone methides with sulfonium or ammonium bromides has been described. This domino-type process offered an efficient method for the synthesis of 2,3-dihydrobenzofurans in good yields, exhibiting good functional group tolerance, scalability and high diastereoselectivity.

A novel [3 + 3] cycloaddition between in situ formed azaoxyallyl cations and 2-alkenylindoles has been developed. This concise method allows the efficient construction of a series of tetrahydro-β-carbolinones in good yields under mild conditions. Gram-scale experiments and further derivatization of tetrahydro-β-carbolinones highlighted the potential utility of our method.

Cu(i)-Catalyzed oxidative homo-coupling of thiazoline-4-carboxylates with good functional group tolerance has been developed.

A Rh(iii)-catalyzed cyclization of azoles with alkynes has been developed to construct azole-fused-pyridines in good to excellent yields.