Home / Small molecules / Discovery / Technology Platform / Late-Stage Functionalization
Late-Stage Functionalization
The difference between a four-week SAR cycle and a one-week one.
What the technique does
Late-stage functionalization uses highly selective reactions to introduce functional groups onto advanced intermediates under mild, selective conditions, diversifying substitution in a lead structure without rebuilding the synthesis. It also prepares specific targets that conventional routes cannot easily reach.
Reaction types of interest run from C–H alkylation and fluorination through halogenation and oxidation to trifluoromethylation.
An integrated service
- Quantum mechanical analysis of the advanced intermediate, to assess reactivity and regioselectivity for the C–H activation of interest
- Synthesis of key intermediates
- High-throughput processing in our catalysis or photochemistry laboratories
- Rapid parallel LCMS analysis and purification of reaction samples
- QM and DP4-AI assisted structure assignment for complex structures
Knowing where the molecule will react before committing the intermediate is what makes the approach work, because an advanced intermediate is the most expensive material in the program.
References
Moir, M. et al., Expert Opin. Drug Discov., 2019, 14, 1137. Goodman, J. M. et al., Chem. Sci., 2020, 11, 4351.