The Application Of In Situ Generated Hypervalent Iodine Compound In The Reaction Of Cycloetherification

We have developed a new method for the synthesis of2,3-dihydrofurans which are attractive starting materials for the synthesis of highly valuable tetrahydrofurans and important structural units in many natural products and biologically active compounds, which exhibit excellent properties in the treatment of tumour and some central nervous system injury. Our method has apparent advantages, such as non-toxicity, mild reaction conditions and easy handling.First of all, we summarized the applications of the in situ generated hypervalent iodine in the organic synthetic chemistry, especially their applications in the construction of C-O、C-N、C-C bonds. Then we explored a new process of in situ generated hypervalent iodine catalyzed cycloetherification of substituted phenols. We optimized the reaction conditions, and excellent results were achieved for the starting materials bearing various substitution. Furthermore, the reactions finished quickly in30minutes. The mechanism was also proposed. After the in situ generated hypervalent iodines were successfully applied to catalyze the cycloetherification of substituted phenols, they also be used in the cycloetherification of substituted ketones.Our study showed that this novel oxidation system consists of inorganic iodine and oxidant can perform as a green and environm-ental-friendly oxidation system in the reaction of cycloetherification, and provides a new method for the synthesis of2,3-dihydrofurans, which are valuable structural unit in synthetic chemistry.