Hetaryl bromides and iodides bearing SO2F group are versatile substrates for metal catalyzed crosscoupling reactions. Due to the high energy of the S–F bond, sulfonyl fluorides are stable toward hydrolysis, metal catalysis, or reductive reaction conditions. On the other hand, they undergo selective nucleophilic substitution at the sulfur(VI) electrophilic center under controllable reaction conditions. Herein we have designed and synthesized a library of bifunctional building blocks for drug design. You can look through structures and design scheme at MedChem Highlights section of our webpage.