Synthesis of 3-iodobenzo[b]thiophenes via iodocyclization/etherification reaction sequence

An efficient method was developed for the synthesis of benzo[b]thiophene core structure using a two-step, multicomponent reaction resulting in favorable yields. This convergent reaction requires room temperature thus eliminating the harsh reaction conditions usually associated with the synthesis of benzo[b]thiophene ring structures. Used in many drugs that treat conditions such as osteoporosis, asthma, and fungal infections, the benzo[b]thiophene core structure is of extreme importance to medicinal and pharmaceutical research. The key step in this process involves the use of an iodine as a cyclizing agent that acts simultaneously as a catalyst. Alcohols such as alkyl, allyl, propargyl, and benzylic are employed to prepare a diverse library of 3-iodobenzo[b]thiophenes.