The α‐iodination of carbonyl compounds is one of the most important procedures in synthetic organic chemistry. These compounds are important precursors for carbon‐carbon, carbon‐oxygen, and carbon‐nitrogen bond formation as well as they are useful for the synthesis of various biologically important heterocyclic compounds. Despite the availability of numerous methods for the synthesis of this important class of compounds, the desired products usually suffering from some impurities such as di‐iodinated or ring iodinated products are formed in the reaction mixture. Therefore, as the essential productivity issues as well as environmental anxieties that need to be addressed to overcome this issue. In this regards, iodine (I2) and N‐iodosuccinimide (NIS) are important reagents for the production of such an important class of intermediates. In recent years considerable advances have been made for the synthesis of α‐iodo carbonyl compounds with high selectivity and purity. In this present review, we have summarized various protocols for the synthesis of α‐iodo carbonyl compounds.
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