C-H Activation to Diversify Lead Compounds

Optimization of drug candidates involves long and difficult syntheses in order to explore new structures. The typical building block strategy and heterocycle chemistry have limitations that leave many structure positions unexplored. In this contest, C-H activation chemistry is becoming the efficient tool to perform late stage modification of lead compound. The exploitation of previously considered inert C-H bonds as new anchor position allows  introduce variety of chemical moieties. Using our platform it is possible to perform one step modification of lead compounds. Depending on the chemistry, modifications include hydroxylation, methoxylation, acetoxylation, or even fluorination.

This versatility is obtained with different catalysts using Mn, Fe, Pd or Rh.

 

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