The design of chiral ligands is the key to attaining high asymmetric induction in transition-metal-catalyzed reactions. Subtle changes in the conformational, steric, and/or electronic properties of the chiral ligand can often lead to dramatic variation of the reactivity and enantioselectivity. As a result of strong substrate dependence in most cases, tunable and readily synthesized ligands are desirable to obtain high enantioselectivities.Nowadays, asymmetric copper-catalyzed conjugate addition and allylic substitution are well-developed methodologies for creating CÀC bonds. Many efforts have been made in designing efficient systems and identifying new ligands to improve enantioselectivities.

The design of chiral ligands is the key to attaining high asymmetric induction in transition-metal-catalyzed reactions. Subtle changes in the conformational, steric, and/or electronic properties of the chiral ligand can often lead to dramatic variation of the reactivity and enantioselectivity. As a result of strong substrate dependence in most cases, tunable and readily synthesized ligands are desirable to obtain high enantioselectivities.Nowadays, asymmetric copper-catalyzed conjugate addition and allylic substitution are well-developed methodologies for creating CÀC bonds. Many efforts have been made in designing efficient systems and identifying new ligands to improve enantioselectivities.

The first use of the NH S-trifluoromethyl sulfoximine as an ortho directing group is described for the functionalization of the aryl group bonded to the sulfur atom. Various electrophiles (halogen, carbon, oxygen, sulfur, boron, etc.) are introduced on the aromatic ring. Cyclic S-trifluoromethyl sulfoximines are synthesized either with properly chosen electrophiles or by structural adjustment of o-azido sulfoximines. Fluorinated analogues of prazosin are also prepared.