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Some N-alkyl phthalimides and saccharin derivatives are important in medicinal chemistry. These compounds can act as antipsychotic, anti-inflammatory and lipid lowering agents, among others. Furthermore, saccharin derivatives can complex with various metal ions, such as Mg2+, Ca2+, Sr2+, Pd2+, Cu2+. One of the most important reactions in synthetic organic chemistry is the conjugate addition of nucleophilic species to the β-carbon of α,β-unsaturated systems. This process allows the construction of carbon backbones it is very valuable from a synthetic point of view. Several attempts in the generation of β-amino derivatives have been reported and the aza-Michael addition reaction is widely recognized as one of the most important carbon-nitrogen bond–forming reaction in organic synthesis. Most of these products have special properties. For instance, the β-amino acids that can be obtained from aza-Michael additions between amines and α,β-unsaturated esters are attractive precursors in preparation of a variety of bioactive molecules and backbone of a variety of drugs. Moreover, the synthesis of β-amino esters has gained considerable attention due to the possibility of generate intermediates for the synthesis of natural products, aminoalcohols, diamines, β-lactams, β-amino acid derivatives and other molecules containing nitrogen. Thus, this reaction provides a simple and appealing route toward synthesis of N-alkyl derivatives of these compounds. In this work, we propose to study the aza-Michael reaction under microwave condition between saccharine and phtalimide with enantiomerically pure diesters of BINOL and TADDOLs derivatives. This methodology allowed us to obtain di-addition products of great synthetic interest with good yields and relatively short reaction times.

Michael Addition of Phthalimide and Saccharin to Enantiomerically Pure Diesters of BINOL and TADDOLs Derivatives Under Microwave Conditions