Abstract The structure of the antiinflammatory drug flurbiprofen [2-(2-fluoro-4-biphenylyl) propionic acid] presents a simple but challenging target to practice regiocontrolled assembly of molecular subunits through optionally site-controlled metalation. The short and efficacious sequence shown leads to the final product: a four-step, one-pot conversion of 3- fluorotoluene into 2-fluoro-4-methylbiphenyl (79%), consecutive deprotonation and ...