Study On The Regioselective C5-H Direct Iodination Of Indoles

This thesis studies the synthesis of 5-iodoindole compounds.The thesis is divided into two chapters:Chapter 1 Progress in the functionalization of indole ringIndoles constitute privileged structures in natural products,pharmaceuticals,agrochemicals,and material science.As a consequence,the functionalization of indoles has been one of the major studied objectives for over one hundred years.Due to the high nucleophilic activity of the pyrrole side of the indole,the functionalization of the indole at the C3 or C2 position has been successfully achieved,and there are many reports in the literature.However,the positional selective functionalization on the benzenoid core of indole has remained a great challenge.This chapter summarizes the previous research on the functionlization of indole ring at each position.Chapter 2 Study on indole at C5 position Selective IodinationNevertheless,to data,the report on direct functionalizing indole at C5 position is rather limited in the literature although C5 linkage of indole is widespread.More regretfully,there is a lack of a general and efficient strategy for the functionalization of indole at the C5 position so far.This chapter discloses regioselective C5 iodination of indoles.The method is characterized by simple operation,wide substrate scopoe,good compatibility of functional groups,high efficiency,and green chemistry.It not only provides a general synthetic strategy for the construction of C5 functional indole,but also offers a concise pathway for the preparation of C5 iodinated indole bioactive substances.