Efficient Hydration Reaction of Internal Alkynes‐to‐Aryl Ketones‐Mediated by the I 2 /S─H System

Abstract The hydration reaction of internal alkynes mediated by I 2 /S─H system has been developed, providing a simple strategy for the preparation of aryl ketones. The I 2 /S─H system exhibited good functional group tolerance to internal alkyne substrates, and various aryl ketones have been obtained in high yields. Although both electronic and steric hindrance effects have a significant impact on the regioselectivity of asymmetric alkyne hydration reactions, steric hindrance plays a dominant role in the regioselectivity of the reaction.