Fluoro-tert-Butyl Groups

The tert-butyl group is one of the most common aliphatic substituents, appearing in over 50 FDA-approved drugs. Fluorination introduces subtle changes in molecular volume while conferring multiple advantages, such as reduced lipophilicity, improved metabolic stability, and lowered pK_a of neighboring functional groups. Since 2023, the groups of O’Hagan and Grygorenko (at Enamine) introduced the β,β,β-trifluoro-tert-butyl moiety, completing the series of mono-/di-/tri-fluoromethyl analogues. Explore our diverse collection of fluoro-tert-butyl compounds to engineer your bioactive molecules!