A novel modular approach to access trifluoromethyl-bearing five-membered ring structure

Trifluoromethyl-bearing five-membered ring structures are widely present in newly designed drugs, but effective methods to access them remain scarce. We developed a new modular approach to obtain a wide range of trifluoromethyl-containing five-membered ring structures via catalytic carbene insertion into C-H bond

• A novel modular approach to trifluoromethyl-bearing 5-membered ring structures via C-H bond activation has been developed.
• The use of perfluorophthalimide-based ligands is the key to achieve enantioselectivity.

• This trifluoromethylation strategy shows high site-, diastereo- and enantioselectivity, with good product yield.
• Chiral CF3 analogues of bioactive molecules can be prepared with this method.
• The use of toxic fluoroalkyl-diazo compounds can be avoided.

• Synthesis of potentially pharmaceutically active molecules containing trifluoromethyl-bearing five-membered ring structures.