CH Functionalization Tool Box
Lead diversification is becoming an viable alternative to de novo synthesis as C-H functionalization chemistry offers many possible transformations including hydroxylation, acetoxylation, methoxylation, and halogenation among others. However each desired transformation can quickly become a mini research problem in and of itself, when the end goal is to quickly acquire the analogue for testing. A real world drug program does not have the time to develop new reaction conditions in order to make analogues that ultimately may not be active.
Our novel and effective lead diversification tool box addresses all these issues by offering a rapid, practical, and cost-effective solution for analogue generation. This approach permits the parallel screening of a selected set of catalytic conditions focusing on generating diversity in an approach which is totally orthogonal and complementary to conventional synthetic methods.