Study On Constructions Of 3-acyl Imiazo [1,2-?] Pyridine With Hypervalent Iodine Generated In Situ

Herein,we have explored the applications of in situ generated hypervalent iodine,in organic synthesis,which was defined as a research of compounds containing high valence iodine generated from low valence iodine of 0 or-1.This paper consists of three sections,the main contents have been shown as below.1?We have summarized research advance in recent years in organic synthesis using in situ generated hypervalent iodine,which provides an efficient access to avoid some problems,such as the requirement of stoichiometric loading of hypervalent iodine,high unstability of hypervalent iodine and easy to explosive with shocking,usually encountered in the reactions with stoichiometric hypervalent iodine.In addition,the principal applications of this strategy to ?-functionalization of ketone carbonyl compounds were described.2?Briefly summarizing the constructions of heterocyclic proceeded via alkenes or alkynes difunctionalization and our study results were also reported.One-step synthesis of 3-acyl imiazo[1,2-?]pyridine proceeded smoothly using alkynyl derivatives as substrates,I2 as catalyst and H2O2 as co-oxidant in undried toluene as well as screening of reaction condition has been conducted.With optimized conditions in hand,we have also investigated the scope of substrates compatibility and explored the plausible mechanism.3?Briefly summarizing the research advance of synthesis of imiazo[1,2-?]pyridine and our study results were also reported.The protocol to facilitate efficient conversion of ?-aminoketones to 3-acyl imiazo[1,2-?]pyridine,which was realized using I2 as catalyst and TBHP as co-oxidant under neat conditions,as well as screening of reaction condition has been conducted.With optimized conditions in hand,we have also investigated the scope of substrates compatibility and explored the plausible mechanism.