Aza-Michael Addition of Imidazole Analogues

This review summarizes methods of N-functionalization of imidazole and its derivatives through simple aza-Michael addition. Apart from advances in the development of efficient additives applied for this transformation, examples of this reaction’s applicability in the synthesis of biologically relevant molecules are presented. 1 Introduction 2 Method Development for Aza-Michael Addition of Imidazole Analogues­ 2.1 Reactions Promoted by Catalysts 2.2 Aza-Michael Addition on Solid Support 2.3 Reactions Promoted by Base 2.4 Reactions Catalyzed by Enzymes 2.5 Reaction Promoted by Ionic Liquids 2.6 Microwave-, Pressure-, and Ultrasound-Assisted Aza-Michael Addition­ 2.7 Asymmetric Aza-Michael Addition 3. Applications of Aza-Michael Addition 3.1 Addition to Doubly Activated Michael Acceptors; Side Reactions 3.2 Synthesis of Amino Acids Using Aza-Michael Addition 3.3 Domino Transformations Including Aza-Michael Addition 3.4 Application of Aza-Michael Addition in the Synthesis of Biologically­ Relevant Compounds 4 Conclusions