A simple and facile iodination method of didechlorotiacumicin B and aromatic compounds

Tiacumicin B (also known as fidaxomicin or difimicin) is a marketed 18-membered macrolide antibiotic for the treatment of Clostridium difficile infections. Tiacumicin B is structurally characterized with two chlorine atoms substituted on the aromatic ring, which is installed by the halogenase TiaM. During the study on halide compatibility of TiaM, a facile and nonenzymatic iodination method of didechlorotiacumicin B was discovered, requiring NaI, acid and air for iodination at room temperature. This method was also amenable to other 9 aromatic substrates with electron-rich sites for iodination.