JSPEN
Nice idea. might be primed to eliminate though and epimerise at chiral centre.
Add an F to the alpha carbon?
Nice idea. might be primed to eliminate though and epimerise at chiral centre.
Add an F to the alpha carbon?
The racemization risk associated with the chiral center would be a big worry. I am not convinced that locking the substituent into an axial orientation will result in significant potency gains and this discussion of the EDJ-MED-e4b030d8 submission may be relevant. I believe that the configuration of the chiral center will need to be locked in order for the dihydrobenzopyrans to be taken forward. Elimination of HF is a potential risk associated with aliphatic fluoro substituents.