1-Bromo-2-chloro-4-fluorobenzene (CAS number 110407-59-5) is derived from benzene, bearing bromide, chloride and fluoride substituents. 1-Bromo-2-chloro-4-fluorobenzene serves as a crucial building block for synthesizing brilanestrant, a selective estrogen receptor degrader used in the treatment of breast cancer. 1-Bromo-2-chloro-4-fluorobenzene controls the potency on the degradation of estrogen receptor 1 (ERα), demonstrating an effective concentration of 0.7 nM.
1-Bromo-2-chloro-4-fluorobenzene is also used in the preparation of a biphenyl catalyst for peptide synthesis. The preparation of the catalyst begins with the synthesis of the Grignard reagent of 1-bromo-2-chloro-4-fluorobenzene yielding a magnesium bromide analog. The resulting product subsequently reacts with trimethyl borate, followed by an acid hydration. The boronic acid product shows high catalytic efficiency of peptide synthesis, achieving a 97% conversion over a 4-hour reaction.