A highly chemo-, diastereo-, and enantioselective Cu(I)/(S,S)-ⁱPr-FOXAP-catalyzed Michael addition of ketiminoester to β-trifluoromethyl β,β-disubstituted enones was developed. This method provides facile access to highly functionalized 1-pyrrolines bearing two contiguous stereocenters, including a trifluoromethylated all-carbon quaternary stereocenter, via one-pot hydrolytic cyclization (up to >20 : 1 cr, > 20 : 1 dr, and 98% ee). The addition of trace amounts of water to the direct 1,3-dipolar cycloaddition is crucial for obtaining 1-pyrrolines with high chemoselectivities rather than pyrrolidines.

Herein, we report a highly diastereo- and enantioselective copper-catalyzed remote asymmetric yne-allylic substitution of yne-allylic esters and thiazolones.

Steroids are widely abused due to their ability to promote protein synthesis, enhance muscle growth, and improve athletic performance, leading to significant unfair competition. This review aims to provide scientific support for anti-doping.

The present work provides efficient access to chiral cyclic 1,2-bis(diphenylphosphino)ethanes (DPPEs) directly from diphosphine oxide alkenes and azomethine ylides via asymmetric [3 + 2] cycloaddition. Both enantiomers of the products can be obtained in good to excellent diastereo- and enantioselectivities (up to >20 : 1 dr and 99% ee). Mild conditions, gram-scale experiment, diverse transformations and preliminary catalytic applications of the DPPEs make this approach highly attractive.