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

LSCCB
Overview

Laboratory for Synthetic Chemistry and Chemical Biology Limited (LSCCB) has developed a novel modular approach to access a wide range of potentially pharmaceutically active molecules containing trifluoromethyl-bearing five-membered ring structures via catalytic carbene insertion into C-H bond

  • A novel modular approach to access  trifluoromethyl-bearing five-membered ring structure 0
Technical name of innovation
A modular approach to trifluoromethyl-bearing 5-membered ring structures via C-H bond activation
Commercialisation opportunities
Collaborative projects on research and development
Problem addressed

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

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

Laboratory for Synthetic Chemistry and Chemical Biology (LSCCB) is an R&D centre funded by Health@InnoHK progamme of Innovation and Technology Commission of  HKSAR. Established in 2020, LSCCB is operated with tripartite joint collaboration of The University of Hong Kong, Imperial College London and Peking University. LSCCB aims at integrating chemical and biomedical sciences to develop new molecular medicines and diagnostic tools for the treatment and analysis of human diseases, in particular, cancer. LSCCB currently assembles more than 20 principal investigators for 4 major research programmes including (a) Synthetic Chemistry; (b) Chemical Biology of Natural Products and Chinese Medicine; (c) Metal Anticancer Medicine, Diagnostics and Theranostics; and (d) Multi-Omics and Innovative Analytical Technologies for InnoHealth.

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